Protein Information

Name Acetylcholinesterase
Synonyms ACHE; ACHE protein; AChE; ARACHE; AcChoEase; Acetylcholine acetylhydrolase; Acetylcholinesterase; Acetylcholinesterase isoform E4 E6 variant…

Compound Information

Name chlorpyrifos
CAS

Reference List

PubMed Abstract RScore(About this table)
17467020 Kaushik R, Rosenfeld CA, Sultatos LG: Concentration-dependent interactions of the organophosphates chlorpyrifos oxon and methyl paraoxon with human recombinant acetylcholinesterase. Toxicol Appl Pharmacol. 2007 Jun 1;221(2):243-50. Epub 2007 Mar 24.

Collectively, these results demonstrate that the interactions of chlorpyrifos oxon and methyl paraoxon with acetylcholinesterase cannot be described by simple Michaelis-Menten kinetics but instead support the hypothesis that these oxons bind to a secondary site on acetylcholinesterase, leading to activation/inhibition of the catalytic site, depending on the nature of the substrate and inhibitor.
145(1,3,3,5) Details
7541841 Carr RL, Straus DL, Chambers JE: Inhibition and aging of channel catfish brain acetylcholinesterase following exposure to two phosphorothionate insecticides and their active metabolites. J Toxicol Environ Health. 1995 Jul;45(3):325-36.

The similar patterns of inhibition, recovery, and aging between the two oxon treatments, which have similar lipophilicities, suggest that the greater amount of AChE inhibition and aging observed in the chlorpyrifos-treated fish compared with the parathion-treated fish probably results from the higher lipophilicity of chlorpyrifos than of parathion.
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17597270 Tyler Mehler W, Schuler LJ, Lydy MJ: Examining the joint toxicity of chlorpyrifos and atrazine in the aquatic species: Lepomis macrochirus, Pimephales promelas and Chironomus tentans. Environ Pollut. 2008 Mar;152(1):217-24. Epub 2007 Jun 26.

In addition, acetylcholinesterase (AChE) inhibition and biotransformation were investigated to evaluate the toxic mode of action of chlorpyrifos in the presence of atrazine.
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8599033 Barron MG, Woodburn KB: Ecotoxicology of chlorpyrifos. . Rev Environ Contam Toxicol. 1995;144:1-93.

Chlorpyrifos is a broad-spectrum organophosphorothioate insecticide with a principal mechanism of toxicity by inactivation of acetylcholinesterase at nerve junctions.
81(1,1,1,1) Details
18447001 Cho TM, Rose RL, Hodgson E: The effect of chlorpyrifos-oxon and other xenobiotics on the human cytochrome P450-dependent metabolism of naphthalene and deet. Drug Metabol Drug Interact. 2007;22(4):235-62.

Chlorpyrifos-oxon (CPO), a metabolite of chlorpyrifos, is a potent inhibitor of acetylcholinesterase and, although the neurotoxicological impact of this organophosphorus compound has been broadly studied both in vitro and in vivo, there are few studies of metabolic interactions of CPO with other xenobiotics.
81(1,1,1,1) Details
17723768 Arduini F, Ricci F, Tuta CS, Moscone D, Amine A, Palleschi G: Detection of carbamic and organophosphorous pesticides in water samples using a cholinesterase biosensor based on Prussian Blue-modified screen-printed electrode. Anal Chim Acta. 2006 Nov 24;580(2):155-62. Epub 2006 Jul 29.

AChE-based biosensors have demonstrated a higher sensitivity towards aldicarb (50% inhibition with 50 ppb) and carbaryl (50% inhibition with 85 ppb) while BChE biosensors have shown a higher affinity towards paraoxon (50% inhibition with 4 ppb) and chlorpyrifos-methyl oxon (50% inhibition with 1 ppb).
32(0,1,1,2) Details
10593083 Pasteur N, Marquine M, Ben Cheikh H, Bernard C, Bourguet D: A new mechanism conferring unprecedented high resistance to chlorpyrifos in Culex pipiens (Diptera: Culicidae). J Med Entomol. 1999 Nov;36(6):794-802.

Chlorpyrifos resistance in the G strain was caused by a major gene (or group of genes) tightly linked to the Ace-1 gene (coding AChE-1 enzyme).
32(0,1,1,2) Details
12216825 Gatti SS, Henderson G, Abdel-Aal YA, Ibrahim SA: Acetylcholinesterase mediated susceptibility of soldiers and workers of formosan subterranean termite (Isoptera: Rhinotermitidae) to chlorpyrifos. J Econ Entomol. 2002 Aug;95(4):813-9.
144(1,3,3,4) Details
11460676 Steevens JA, Benson WH: Interactions of chlorpyrifos and methyl mercury: a mechanistic approach to assess chemical mixtures. Mar Environ Res. 2000 Jul-Dec;50(1-5):113-7.

The formation of this complex may result in increased accumulation of methyl mercury, apparent additive toxicity, and protection against chlorpyrifos-mediated acetylcholinesterase inhibition.
143(1,3,3,3) Details
14691213 Caughlan A, Newhouse K, Namgung U, Xia Z: Chlorpyrifos induces apoptosis in rat cortical neurons that is regulated by a balance between p38 and ERK/JNK MAP kinases. Toxicol Sci. 2004 Mar;78(1):125-34. Epub 2003 Dec 22.

It is generally agreed that chlorpyrifos-oxon is approximately three orders of magnitude more potent than chlorpyrifos in inhibition of brain acetylcholinesterase activity.
143(1,3,3,3) Details
17018647 Kousba AA, Poet TS, Timchalk C: Age-related brain cholinesterase inhibition kinetics following in vitro incubation with chlorpyrifos-oxon and diazinon-oxon. Toxicol Sci. 2007 Jan;95(1):147-55. Epub 2006 Oct 3.

Chlorpyrifos and diazinon are two commonly used organophosphorus insecticides (OPs), and their primary mechanism of action involves the inhibition of acetylcholinesterase by their metabolites chlorpyrifos-oxon (CPO) and diazinon-oxon (DZO), respectively.
81(1,1,1,1) Details
19476409 Vioque-Fernandez A, de Almeida EA, Lopez-Barea J: Biochemical and proteomic effects in Procambarus clarkii after chlorpyrifos or carbaryl exposure under sublethal conditions. Biomarkers. 2009 Aug;14(5):299-310.

Chlorpyrifos inhibited carboxylesterase activity in a concentration-dependent manner, but acetylcholinesterase was less sensitive.
81(1,1,1,1) Details
17321052 Prendergast MA, Self RL, Smith KJ, Ghayoumi L, Mullins MM, Butler TR, Buccafusco JJ, Gearhart DA, Terry AV Jr: Microtubule-associated targets in chlorpyrifos oxon hippocampal neurotoxicity. Neuroscience. 2007 Apr 25;146(1):330-9. Epub 2007 Feb 22.

The present studies examined effects of prolonged exposure to chlorpyrifos oxon (CPO) on acetylcholinesterase (AChE) activity, immunoreactivity (IR) of microtubule-associated proteins, neuronal injury, and tubulin polymerization using in vitro organotypic slice cultures of rat hippocampus and bovine tubulin.
32(0,1,1,2) Details
18393628 Hoogduijn MJ, Cheng A, Genever PG: Functional Nicotinic and Muscarinic Receptors on Mesenchymal Stem Cells. . Stem Cells Dev. 2008 Mar 10.

The acetylcholinesterase inhibitor chlorpyrifos, which is widely used as an agricultural insecticide, had similar effects on intracellular Ca2+ and cAMP in MSCs.
32(0,1,1,2) Details
19699221 Shenouda J, Green P, Sultatos L: An evaluation of the inhibition of human butyrylcholinesterase and acetylcholinesterase by the organophosphate chlorpyrifos oxon. Toxicol Appl Pharmacol. 2009 Dec 1;241(2):135-42. Epub 2009 Aug 19.

In contrast to inhibition of butyrylcholinesterase, inhibition of human acetylcholinesterase by chlorpyrifos oxon in vitro followed concentration-dependent inhibition kinetics, with the k (i) increasing as the inhibitor concentration decreased.
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15751007 Venkateswara Rao J, Parvathi K, Kavitha P, Jakka NM, Pallela R: Effect of chlorpyrifos and monocrotophos on locomotor behaviour and acetylcholinesterase activity of subterranean termites, Odontotermes obesus. Pest Manag Sci. 2005 Apr;61(4):417-21.

In vitro studies indicated that the I50 value (50% inhibition) for chlorpyrifos against AChE was 8.75 times that of monocrotophos.
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18761328 Mirajkar N, Pope CN: In vitro sensitivity of cholinesterases and [3H] oxotremorine-M binding in heart and brain of adult and aging rats to organophosphorus anticholinesterases. Biochem Pharmacol. 2008 Oct 15;76(8):1047-58. Epub 2008 Aug 12.

In the heart, butyrylcholinesterase was markedly more sensitive than acetylcholinesterase to inhibition by chlorpyrifos oxon, and butyrylcholinesterase in tissues from aging rats was more sensitive than enzyme from adults, possibly due to differences in A-esterase mediated detoxification.
114(1,2,2,4) Details
10630569 Steevens JA, Benson WH: Toxicological interactions of chlorpyrifos and methyl mercury in the amphipod, Hyalella azteca. Toxicol Sci. 1999 Dec;52(2):168-77.

The formation of this complex may result in increased accumulation of methyl mercury, apparent additive toxicity, and protection against chlorpyrifos mediated acetylcholinesterase inhibition.
113(1,2,2,3) Details
17893397 Betancourt AM, Filipov NM, Carr RL: Alteration of neurotrophins in the hippocampus and cerebral cortex of young rats exposed to chlorpyrifos and methyl parathion. Toxicol Sci. 2007 Dec;100(2):445-55. Epub 2007 Sep 24.

Exposure to either chlorpyrifos (CPS) or methyl parathion (MPS) results in the inhibition of acetylcholinesterase and leads to altered neuronal activity which normally regulates critical genes such as the neurotrophins nerve growth factor (NGF) and brain-derived neurotrophic factor (BDNF).
81(1,1,1,1) Details
18456295 Jortner BS: Effect of stress at dosing on organophosphate and heavy metal toxicity. . Toxicol Appl Pharmacol. 2008 Nov 15;233(1):162-7. Epub 2008 Mar 18.

Chlorpyrifos (single 60 mg/kg subcutaneously) elicited marked inhibition of brain acetylcholinesterase 4-day post-dosing.
81(1,1,1,1) Details
20350560 Moreira EG, Yu X, Robinson JF, Griffith W, Hong SW, Beyer RP, Bammler TK, Faustman EM: Toxicogenomic profiling in maternal and fetal rodent brains following gestational exposure to chlorpyrifos. Toxicol Appl Pharmacol. 2010 Mar 26.

Considering the wide variety of effects that have been reported to occur in the developmental neurotoxicity of chlorpyrifos (CP) and the lack of consensus on their dependence of brain acethylcholinesterase (AChE) activity inhibition, we applied microarray technology to explore dose-dependent alterations in transcriptional response in the fetal and maternal C57BL/6 mouse brain after daily gestational exposure (days 6 to 17) to CP (2, 4, 10, 12 or 15mg/kg, sc).
32(0,1,1,2) Details
11275418 Bomser JA, Casida JE: Diethylphosphorylation of rat cardiac M2 muscarinic receptor by chlorpyrifos oxon in vitro. Toxicol Lett. 2001 Feb 3;119(1):21-6.

The acute toxicity of chlorpyrifos oxon (CPO), the metabolically-activated form of the major organophosphorus insecticide chlorpyrifos, is attributable to diethylphosphorylation of acetylcholinesterase at its esteratic site.
31(0,1,1,1) Details
19477011 Kienle C, Kohler HR, Gerhardt A: Behavioural and developmental toxicity of chlorpyrifos and nickel chloride to zebrafish (Danio rerio) embryos and larvae. Ecotoxicol Environ Saf. 2009 Sep;72(6):1740-7. Epub 2009 May 23.

Chlorpyrifos is an acetylcholine esterase inhibitor, which is likely to affect behaviour of the organism.
31(0,1,1,1) Details
17366821 Jameson RR, Seidler FJ, Slotkin TA: Nonenzymatic functions of acetylcholinesterase splice variants in the developmental neurotoxicity of organophosphates: chlorpyrifos, chlorpyrifos oxon, and diazinon. Environ Health Perspect. 2007 Jan;115(1):65-70.

OBJECTIVES: We exposed differentiating PC12 cells, a model for developing neurons, to 30 microM chlorpyrifos (CPF) or diazinon (DZN), or CPF oxon, the active metabolite that irreversibly inhibits AChE enzymatic activity, in order to determine whether they differentially induce the formation of AChE-S as a mechanistic predictor of developmental neurotoxicity.
119(1,2,2,9) Details
20020880 Tuzmen MN, Candan N, Kaya E: The evaluation of altered antioxidative defense mechanism and acetylcholinesterase activity in rat brain exposed to chlorpyrifos, deltamethrin, and their combination. Toxicol Mech Methods. 2007;17(9):535-40.

Biochemical analysis showed that administration of chlorpyrifos and deltamethrin causes brain damage via production of MDA and inhibition of AChE.
118(1,2,3,3) Details
15036870 Buchwalter DB, Sandahl JF, Jenkins JJ, Curtis LR: Roles of uptake, biotransformation, and target site sensitivity in determining the differential toxicity of chlorpyrifos to second to fourth instar Chironomous riparius (Meigen). Aquat Toxicol. 2004 Feb 10;66(2):149-57.

In vitro acetylcholinesterase (AChE) assays were performed with chlorpyrifos and the metabolite, chlorpyrifos-oxon, to investigate potential target site sensitivity differences among instars.
100(1,1,4,5) Details
7537966 Chiappa S, Padilla S, Koenigsberger C, Moser V, Brimijoin S: Slow accumulation of acetylcholinesterase in rat brain during enzyme inhibition by repeated dosing with chlorpyrifos. Biochem Pharmacol. 1995 Mar 30;49(7):955-63.
97(1,1,3,7) Details
11386720 Doran WJ, Gregory Cope W, Rada RG, Sandheinrich MB: Acetylcholinesterase inhibition in the threeridge mussel (Amblema plicata) by chlorpyrifos: implications for biomonitoring. Ecotoxicol Environ Saf. 2001 May;49(1):91-8.
96(1,1,3,6) Details
16243090 Eddleston M, Eyer P, Worek F, Mohamed F, Senarathna L, von Meyer L, Juszczak E, Hittarage A, Azhar S, Dissanayake W, Sheriff MH, Szinicz L, Dawson AH, Buckley NA: Differences between organophosphorus insecticides in human self-poisoning: a prospective cohort study. Lancet. 2005 Oct 22-28;366(9495):1452-9.

Acetylcholinesterase inhibited by fenthion or dimethoate responded poorly to pralidoxime treatment compared with chlorpyrifos-inhibited acetylcholinesterase.
81(1,1,1,1) Details
18222074 Yu F, Wang Z, Ju B, Wang Y, Wang J, Bai D: Apoptotic effect of organophosphorus insecticide chlorpyrifos on mouse retina in vivo via oxidative stress and protection of combination of vitamins C and E. Exp Toxicol Pathol. 2008 Apr;59(6):415-23. Epub 2008 Jan 25.

Moreover, chlorpyrifos treatment inhibited acetylcholinesterase activity and promoted [Ca (2+)](i) level in mouse retinal cells, which were also attenuated by combination of vitamins C and E.
81(1,1,1,1) Details
10355543 Jett DA, Navoa RV, Lyons MA Jr: Additive inhibitory action of chlorpyrifos and polycyclic aromatic hydrocarbons on acetylcholinesterase activity in vitro. Toxicol Lett. 1999 Apr 12;105(3):223-9.
69(0,2,2,9) Details
19159775 Istamboulie G, Fournier D, Marty JL, Noguer T: Phosphotriesterase: a complementary tool for the selective detection of two organophosphate insecticides: chlorpyrifos and chlorfenvinfos. Talanta. 2009 Mar 15;77(5):1627-31. Epub 2008 Oct 14.

This work shows the possibility of combining the high sensitivity of genetically-modified Drosophila melanogaster acetylcholinesterase (B394) with the ability of phosphotriesterase (PTE) to hydrolyse organophosphate compounds, in the aim of developing a biosensor selective to two insecticides of interest: chlorpyrifos and chlorfenvinfos.
31(0,1,1,1) Details
10544056 Das KP, Barone S Jr: Neuronal differentiation in PC12 cells is inhibited by chlorpyrifos and its metabolites: is acetylcholinesterase inhibition the site of action?. Toxicol Appl Pharmacol. 1999 Nov 1;160(3):217-30.
115(1,2,2,5) Details
8806854 Carr RL, Chambers JE: Kinetic analysis of the in vitro inhibition, aging, and reactivation of brain acetylcholinesterase from rat and channel catfish by paraoxon and chlorpyrifos-oxon. Toxicol Appl Pharmacol. 1996 Aug;139(2):365-73.

The higher association constant (KA) of chlorpyrifos-oxon than paraoxon in both species and the lack of significant differences in the phosphorylation constants (kp) suggest that association of the inhibitor with AChE is the principal factor in the different potencies between these two inhibitors.
114(1,2,2,4) Details
16838488 Musilek K, Kuca K, Jun D, Dohnal V, Kim TH, Jung YS, Dolezal M: [Synthesis of reactivators of phosphorylated acetylcholinesterase of bis-pyridiniumdialdoxime type with a 3-oxapentane connecting chain and their testing in vitro on a model of the enzyme inhibited by chlorpyrifos and methylchlorpyrifos]. Ceska Slov Farm. 2006 May;55(3):115-9.

On the other hand, the known reactivators surpass new substances in the case of chlorpyrifos-inhibited AChE at both concentrations.
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18371683 Kuswandi B, Fikriyah CI, Gani AA: An optical fiber biosensor for chlorpyrifos using a single sol-gel film containing acetylcholinesterase and bromothymol blue. Talanta. 2008 Jan 15;74(4):613-8. Epub 2007 Jul 7.

A linear calibration curve of chlorpyrifos against the percentage inhibition of AChE was obtained from 0.05 to 2.0mg/L of chlorpyrifos (18-80% inhibition, R (2)=0.9869, n=6).
95(1,1,3,5) Details
15893801 Colombo A, Orsi F, Bonfanti P: Exposure to the organophosphorus pesticide chlorpyrifos inhibits acetylcholinesterase activity and affects muscular integrity in Xenopus laevis larvae. Chemosphere. 2005 Dec;61(11):1665-71.
93(1,1,2,8) Details
9465262 Mortensen SR, Brimijoin S, Hooper MJ, Padilla S: Comparison of the in vitro sensitivity of rat acetylcholinesterase to chlorpyrifos-oxon: what do tissue IC50 values represent?. Toxicol Appl Pharmacol. 1998 Jan;148(1):46-9.

AChE IC50 values were determined by incubating tissue homogenates with chlorpyrifos-oxon (active metabolite of chlorpyrifos, a common organophosphate insecticide) for 30 min at 26 degrees C, and then measuring residual AChE activity.
89(1,1,2,4) Details
18266068 Picco EJ, Rubio MR, David DC, Rodriguez C, Boggio JC: Pharmacokinetics and pharmacodynamics of chlorpyrifos in male and female cattle after topical administration. Vet Res Commun. 2008 Jun;32(5):401-10. Epub 2008 Feb 12.

The aim of this work was to study the pharmacokinetic behaviour and the inhibitory effect on acetylcholinesterase and butyrylcholinesterase activities of chlorpyrifos in male and female cattle after pour-on administration.
65(0,2,2,5) Details
12389926 Sandahl JF, Jenkins JJ: Pacific steelhead (Oncorhynchus mykiss) exposed to chlorpyrifos: benchmark concentration estimates for acetylcholinesterase inhibition. Environ Toxicol Chem. 2002 Nov;21(11):2452-8.
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18615705 Yang ML, Zhang JZ, Zhu KY, Xuan T, Liu XJ, Guo YP, Ma EB: Mechanisms of organophosphate resistance in a field population of oriental migratory locust, Locusta migratoria manilensis (Meyen). Arch Insect Biochem Physiol. 2009 May;71(1):3-15.

The susceptibilities to three organophosphate (OP) insecticides (malathion, chlorpyrifos, and phoxim), responses to three metabolic synergists [triphenyl phosphate (TPP), piperonyl butoxide (PBO), and diethyl maleate (DEM)], activities of major detoxification enzymes [general esterases (ESTs), glutathione S-transferases (GSTs), and cytochrome P450 monooxygenases (P450s)], and sensitivity of the target enzyme acetylcholinesterase (AChE) were compared between a laboratory-susceptible strain (LS) and a field-resistant population (FR) of the oriental migratory locust, Locusta migratoria manilensis (Meyen).
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20112867 Somnuek C, Boonphakdee C, Cheevaporn V, Tanaka K: Gene expression of acetylcholinesterase in hybrid catfish (Clarias gariepinus X Clarias macrocephalus) exposed to chlorpyrifos and carbaryl. J Environ Biol. 2009 Jan;30(1):83-8.

Specific primers of the hybrid catfish AChE gene were then synthesized and used in the examination of AChE gene expression in brain tissue of hybrid catfish exposed to sublethal concentrations of chlorpyrifos (0.43, 4.3 and 43 microM) and carbaryl (1.19, 11.9 and 119 microM) for 24 hr.
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17194517 Duysen EG, Li B, Darvesh S, Lockridge O: Sensitivity of butyrylcholinesterase knockout mice to (--)-huperzine A and donepezil suggests humans with butyrylcholinesterase deficiency may not tolerate these Alzheimer's disease drugs and indicates butyrylcholinesterase function in neurotransmission. Toxicology. 2007 Apr 20;233(1-3):60-9. Epub 2006 Dec 2.

We tested this hypothesis by challenging BChE and AChE knockout mice, as well as wild-type mice, with the AChE specific inhibitors, (--)-huperzine A and donepezil, and with serine hydrolase inhibitors, echothiophate and chlorpyrifos oxon. (--)-Huperzine A and donepezil caused mortality and significant toxicity in the BChE-/- animals.
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12651185 Venkateswara Rao J, Surya Pavan Y, Madhavendra SS: Toxic effects of chlorpyrifos on morphology and acetylcholinesterase activity in the earthworm, Eisenia foetida. Ecotoxicol Environ Saf. 2003 Mar;54(3):296-301.

The present study demonstrates a dose- and time-dependent exposure of chlorpyrifos through skin results, morphological abnormalities, and inhibition of AChE in the earthworm, E. foetida.
89(1,1,2,4) Details
14761482 Wu YJ, Sun YJ, Carey P: [Effect of paraoxon and chlorpyrifos on the nicotinic autoreceptor function in rat cortical synaptosomes]. Zhonghua Lao Dong Wei Sheng Zhi Ye Bing Za Zhi. 2003 Jun;21(3):188-90.

Chlorpyrifos markedly reduced NAF by 66% 96 h after treatment and inhibited the AChE activity by 91% in vivo.
87(1,1,2,2) Details
16865602 Rakotondravelo ML, Anderson TD, Charlton RE, Zhu KY: Sublethal effects of three pesticides on activities of selected target and detoxification enzymes in the aquatic midge, Chironomus tentans (diptera: chironomidae). Arch Environ Contam Toxicol. 2006 Oct;51(3):360-6. Epub 2006 Jul 21.

Exposures of midges to chlorpyrifos at 0.10 microg/L for 20 d reduced AChE activity by 59.8%, and GE activities toward the substrates alpha-naphthyl acetate and beta-naphthyl acetate by 30.7 and 48.8%, respectively.
87(1,1,2,2) Details
11332845 Park NJ, Kamble ST: Decapitation impacting effect of topically applied chlorpyrifos on acetylcholinesterase and general esterases in susceptible and resistant German cockroaches (Dictyoptera: Blattellidae). J Econ Entomol. 2001 Apr;94(2):499-505.

Inhibition of isozymes d1 and d2 seems to be more important in chlorpyrifos intoxication than acetylcholinesterase.
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10873710 Monnet-Tschudi F, Zurich MG, Schilter B, Costa LG, Honegger P: Maturation-dependent effects of chlorpyrifos and parathion and their oxygen analogs on acetylcholinesterase and neuronal and glial markers in aggregating brain cell cultures. Toxicol Appl Pharmacol. 2000 Jun 15;165(3):175-83.

Oxon derivatives were more potent AChE inhibitors than the parent compounds, and parathion was more potent than chlorpyrifos.
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10681099 Lesser J, Blodgett D, Ehrich M: Comparison of oxime-initiated reactivation of organophosphorous-inhibited acetylcholinesterase in brains of avian embryos. J Toxicol Environ Health A. 2000 Jan 14;59(1):57-66.

Doses of chlorpyrifos, parathion, acephate, and trichlorfon that inhibited AChE > 70% were administered to the embryos.
87(1,1,1,7) Details
18076960 Yang D, Howard A, Bruun D, Ajua-Alemanj M, Pickart C, Lein PJ: Chlorpyrifos and chlorpyrifos-oxon inhibit axonal growth by interfering with the morphogenic activity of acetylcholinesterase. Toxicol Appl Pharmacol. 2008 Apr 1;228(1):32-41. Epub 2007 Nov 17.
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18617161 Jun D, Musilova L, Kuca K, Kassa J, Bajgar J: Potency of several oximes to reactivate human acetylcholinesterase and butyrylcholinesterase inhibited by paraoxon in vitro. Chem Biol Interact. 2008 Sep 25;175(1-3):421-4. Epub 2008 May 7.

Organophosphorus pesticides (e.g. chlorpyrifos, malathion, and parathion) and nerve agents (sarin, tabun, and VX) are highly toxic organophosphorus compounds with strong inhibition potency against two key enzymes in the human body-acetylcholinesterase (AChE; EC 3.1.1.7) and butyrylcholinesterase (BuChE; EC 3.1.1.8).
86(1,1,1,6) Details
7684990 Richardson RJ, Moore TB, Kayyali US, Fowke JH, Randall JC: Inhibition of hen brain acetylcholinesterase and neurotoxic esterase by chlorpyrifos in vivo and kinetics of inhibition by chlorpyrifos oxon in vitro: application to assessment of neuropathic risk. Fundam Appl Toxicol. 1993 Apr;20(3):273-9.
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16819104 Rao JV, Begum G, Pallela R, Usman PK, Rao RN: Changes in behavior and brain acetylcholinesterase activity in mosquito fish, Gambusia affinis in response to the sub-lethal exposure to chlorpyrifos. Int J Environ Res Public Health. 2005 Dec;2(3-4):478-83.

Sub-lethal studies of chlorpyrifos, O,O-diethyl-O-(3,5,6-trichloro-2-pyridyl) phosphorothioate on mosquito fish, Gambusia affinis were carried out in vivo, for 20 days to assess the locomotor behavior in relation to bioaccumulation and interaction with a targeted enzyme, acetylcholinesterase (AChE, EC: 3.1.1.7).
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19608286 Xuereb B, Lefevre E, Garric J, Geffard O: Acetylcholinesterase activity in Gammarus fossarum (Crustacea Amphipoda): linking AChE inhibition and behavioural alteration. Aquat Toxicol. 2009 Aug 31;94(2):114-22. Epub 2009 Jun 24.

Relations between whole-body acetylcholinesterase (AChE) inhibition and changes in feeding and locomotor behaviours were investigated in adult male Gammarus fossarum during short-term exposure (96h) to the organophosphorous pesticide chlorpyrifos (CPE) and the carbamate pesticide methomyl (MT).
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16363165 Liu H, Xu Q, Zhang L, Liu N: Chlorpyrifos resistance in mosquito Culex quinquefasciatus. J Med Entomol. 2005 Sep;42(5):815-20.

An inhibition study of acetylcholinesterase (AChE) by chlorpyrifos showed that bimolecular rate constants (Ki) of chlorpyrifos for the inhibition of AChE in adults and larvae of the susceptible S-Lab strain were 2.2- and 1.9-fold higher, respectively, than in the HAmCq strain and 3.4- and 3.8-fold higher than in the MAmCq strain.
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19433070 Eyer F, Roberts DM, Buckley NA, Eddleston M, Thiermann H, Worek F, Eyer P: Extreme variability in the formation of chlorpyrifos oxon (CPO) in patients poisoned by chlorpyrifos (CPF). Biochem Pharmacol. 2009 Sep 1;78(5):531-7. Epub 2009 May 9.

Chlorpyrifos oxon (CPO) is the active metabolite of CPF that inhibits acetylcholinesterase.
83(1,1,1,3) Details
20097188 Lee S, Poet TS, Smith JN, Busby-Hjerpe AL, Timchalk C: Effect of in vivo nicotine exposure on chlorpyrifos pharmacokinetics and pharmacodynamics in rats. Chem Biol Interact. 2010 Mar 30;184(3):449-57. Epub 2010 Jan 25.

Chlorpyrifos is an organophosphorus (OP) insecticide that is bioactivated to chlorpyrifos-oxon, and manifests its neurotoxicity by inhibiting acetylcholinesterase (AChE).
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10229710 Bigbee JW, Sharma KV, Gupta JJ, Dupree JL: Morphogenic role for acetylcholinesterase in axonal outgrowth during neural development. Environ Health Perspect. 1999 Feb;107 Suppl 1:81-7.

These results could have additional significance as AChE is the target enzyme of agricultural organophosphate and carbamate pesticides as well as the commonly used household organophosphate chlorpyrifos (Dursban).
37(0,1,1,7) Details
9268605 Ehrich M, Correll L, Veronesi B: Acetylcholinesterase and neuropathy target esterase inhibitions in neuroblastoma cells to distinguish organophosphorus compounds causing acute and delayed neurotoxicity. Fundam Appl Toxicol. 1997 Jul;38(1):55-63.

Inhibition of AChE was greater than inhibition of NTE, without overlap of the concentration-response curves, for OPs which are more likely to cause acute, rather than delayed, neurotoxic effects in vivo (e.g., chlorpyrifos-oxon, dichlorvos, and trichlorfon).
37(0,1,1,7) Details
12020023 Byrne FJ, Toscano NC: Evaluation of peracid activated organophosphates in studies of insecticide resistance conferred by insensitive acetylcholinesterases. J Econ Entomol. 2002 Apr;95(2):425-9.

Incubation of chlorpyrifos and sulprofos with meta-chloroperoxybenzoic acid (MCPBA) produced active metabolites capable of distinguishing between AChE enzymes conferring OP susceptibility and resistance in populations of the tobacco whitefly, Bemisia tabaci Gennadius, and the beet armyworm, Spodoptera exigua Hubner.
83(1,1,1,3) Details
11051590 Goel A, Chauhan DP, Dhawan DK: Protective effects of zinc in chlorpyrifos induced hepatotoxicity: a biochemical and trace elemental study. Biol Trace Elem Res. 2000 May;74(2):171-83.

It was observed that chlorpyrifos (13.5 mg/kg body weight) treatment resulted in significant inhibition (p < 0.001) of serum and hepatic acetylcholinesterase (AChE) activities after 8 wk.
82(1,1,1,2) Details
15036868 Barata C, Solayan A, Porte C: Role of B-esterases in assessing toxicity of organophosphorus (chlorpyrifos, malathion) and carbamate (carbofuran) pesticides to Daphnia magna. Aquat Toxicol. 2004 Feb 10;66(2):125-39.

In this study, the cladoceran Daphnia magna was exposed to two model organophosphorous and one carbamate pesticides including malathion, chlorpyrifos and carbofuran to assess acetylcholinesterase (AChE) and carboxylesterase (CbE) inhibition and recovery patterns and relate those responses with individual level effects.
36(0,1,1,6) Details
9561967 Liu J, Pope CN: Comparative presynaptic neurochemical changes in rat striatum following exposure to chlorpyrifos or parathion. J Toxicol Environ Health A. 1998 Apr 10;53(7):531-44.

Previous studies in our laboratory have demonstrated, however, that dosages of the OPs chlorpyrifos (CPF) or parathion (PS), which cause similar degrees of brain AChE inhibition in adult male rats, can produce marked differences in toxicity.
36(0,1,1,6) Details
15683177 Sandahl JF, Baldwin DH, Jenkins JJ, Scholz NL: Comparative thresholds for acetylcholinesterase inhibition and behavioral impairment in coho salmon exposed to chlorpyrifos. Environ Toxicol Chem. 2005 Jan;24(1):136-45.
332(4,4,5,7) Details
17702992 Sultatos LG: Concentration-dependent binding of chlorpyrifos oxon to acetylcholinesterase. Toxicol Sci. 2007 Nov;100(1):128-35. Epub 2007 Aug 16.
197(2,3,3,7) Details
8954750 Abou-Donia MB, Wilmarth KR, Abdel-Rahman AA, Jensen KF, Oehme FW, Kurt TL: Increased neurotoxicity following concurrent exposure to pyridostigmine bromide, DEET, and chlorpyrifos. Fundam Appl Toxicol. 1996 Dec;34(2):201-22.

In contrast, a significant inhibition of brain acetylcholinesterase (AChE) was produced in hens administered chlorpyrifos alone (activity 67% of control), while those given chlorpyrifos in combination with other compounds exhibited a significant inhibition of brain AChE activity ranging from 43 to 76%.
82(1,1,1,2) Details
12767693 Kousba AA, Poet TS, Timchalk C: Characterization of the in vitro kinetic interaction of chlorpyrifos-oxon with rat salivary cholinesterase: a potential biomonitoring matrix. Toxicology. 2003 Jun 30;188(2-3):219-32.

The primary mechanism of action for organophosphorus (OP) insecticides such as chlorpyrifos (CPF) involves the inhibition of acetylcholinesterase (AChE) by their active oxon metabolites resulting in a wide range of neurotoxic effects.
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16403852 Rosenfeld CA, Sultatos LG: Concentration-dependent kinetics of acetylcholinesterase inhibition by the organophosphate paraoxon. Toxicol Sci. 2006 Apr;90(2):460-9. Epub 2006 Jan 10.

However, more recently certain kinetic complexities in the inhibition of acetylcholinesterase by organophosphates such as paraoxon (O,O-diethyl O-(p-nitrophenyl) phosphate) and chlorpyrifos oxon (O,O-diethyl O-(3,5,6-trichloro-2-pyridyl) phosphate) have raised questions regarding the adequacy of the kinetic scheme on which k (i) is based.
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7689992 Chambers JE, Carr RL: Inhibition patterns of brain acetylcholinesterase and hepatic and plasma aliesterases following exposures to three phosphorothionate insecticides and their oxons in rats. Fundam Appl Toxicol. 1993 Jul;21(1):111-9.

Aliesterases were inhibited to a greater extent than acetylcholinesterase at each sampling time with parathion and chlorpyrifos and their oxons, whereas the reverse was true with methyl parathion and methyl paraoxon.
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7531775 Richardson RJ: Assessment of the neurotoxic potential of chlorpyrifos relative to other organophosphorus compounds: a critical review of the literature. J Toxicol Environ Health. 1995 Feb;44(2):135-65.

Because chlorpyrifos and other OP insecticides are designed to produce acute cholinergic effects through inhibition of acetylcholinesterase (AChE) and some OP compounds can cause OP compound-induced delayed neurotoxicity (OPIDN) via chemical modification of neurotoxic esterase (neuropathy target esterase, NTE), this review focuses on the capacity of chlorpyrifos to precipitate these and other adverse neurological consequences.
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11405414 Abu-Qare AW, Abdel-Rahman A, Brownie C, Kishk AM, Abou-Donia MB: Inhibition of cholinesterase enzymes following a single dermal dose of chlorpyrifos and methyl parathion, alone and in combination, in pregnant rats. J Toxicol Environ Health A. 2001 Jun 8;63(3):173-89.

Chlorpyrifos inhibited maternal and fetal brain acetylcholinesterase (AChE) activity within 24 h of dosing, (48% and 67% of control activity, respectively).
195(2,3,3,5) Details
18775593 Laguerre C, Sanchez-Hernandez JC, Kohler HR, Triebskorn R, Capowiez Y, Rault M, Mazzia C: B-type esterases in the snail Xeropicta derbentina: an enzymological analysis to evaluate their use as biomarkers of pesticide exposure. Environ Pollut. 2009 Jan;157(1):199-207. Epub 2008 Sep 4.

Acetylcholinesterase activity was concentration-dependently inhibited by chlorpyrifos-oxon, dichlorvos, carbaryl and carbofuran (IC50=1.35x10 (-5)-3.80x10 (-8) M).
82(1,1,1,2) Details
11881970 Sachana M, Flaskos J, Nikolaidis E, Hargreaves A, Alexaki-Tzivanidou E: Inhibition of rat platelet 5-hydroxytryptamine uptake by chlorpyrifos and carbaryl. Pharmacol Toxicol. 2001 Oct;89(4):195-200.

In contrast, subacute chlorpyrifos exposure caused a 94.96% inhibition of AChE and a 85.8% inhibition of BuChE and, also, elicited a significant (35.02%) reduction in the platelet uptake of 5-HT.
82(1,1,1,2) Details
7522308 Stanton ME, Mundy WR, Ward T, Dulchinos V, Barry CC: Time-dependent effects of acute chlorpyrifos administration on spatial delayed alternation and cholinergic neurochemistry in weanling rats. Neurotoxicology. 1994 Spring;15(1):201-8.

PND21 exposure to chlorpyrifos produced dose-related inhibition and recovery of brain AChE over the PND24-27 age range.
82(1,1,1,2) Details
16704049 Scholz NL, Truelove NK, Labenia JS, Baldwin DH, Collier TK: Dose-additive inhibition of chinook salmon acetylcholinesterase activity by mixtures of organophosphate and carbamate insecticides. Environ Toxicol Chem. 2006 May;25(5):1200-7.

We extracted AChE from the olfactory nervous system of chinook salmon (Oncorhynchus tshawytscha) and investigated the inhibitory effects of organophosphates (the oxon derivatives of diazinon, chlorpyrifos, and malathion) and carbamates (carbaryl and carbofuran), alone and in two-way combinations.
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16302258 Richter S, Nieveler J, Schulze H, Bachmann TT, Schmid RD: High yield production of a mutant Nippostrongylus brasiliensis acetylcholinesterase in Pichia pastoris and its purification. Biotechnol Bioeng. 2006 Apr 5;93(5):1017-22.

Active site titration with chlorpyrifos, a strong AChE inhibitor, yielded in a specific activity of 3,400 U/mg.
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7513360 Huff RA, Corcoran JJ, Anderson JK, Abou-Donia MB: Chlorpyrifos oxon binds directly to muscarinic receptors and inhibits cAMP accumulation in rat striatum. J Pharmacol Exp Ther. 1994 Apr;269(1):329-35.

The current study verifies that the insecticide O,O-diethyl O-3,5,6-trichloro-2-pyridinyl phosphorothionate (chlorpyrifos) and its oxon metabolite inhibits acetylcholinesterase (AChE).
195(2,3,3,5) Details
10051415 Chen WL, Sheets JJ, Nolan RJ, Mattsson JL: Human red blood cell acetylcholinesterase inhibition as the appropriate and conservative surrogate endpoint for establishing chlorpyrifos reference dose. Regul Toxicol Pharmacol. 1999 Feb;29(1):15-22.
175(1,4,4,5) Details
17265677 Racakova V, Hrabinova M, Jun D, Kuca K: Substituted monoquaternary oximes as reactivators of cyclosarin--and chlorpyrifos--inhibited acetylcholinesterase. Arh Hig Rada Toksikol. 2006 Dec;57(4):387-90.
171(2,2,3,6) Details
20021020 Das GP, Jamil K, Rahman MF: Effect of four organophosphorus compounds on human blood acetylcholinesterase: in vitro studies. Toxicol Mech Methods. 2006;16(8):455-9.

The aim of the study was to determine the IC50 concentration of the pesticides monocrotophos, chlorpyrifos, profenofos, and acephate as inhibitors of AChE.
170(2,2,3,5) Details
11307850 Won YK, Liu J, Olivier K Jr, Zheng Q, Pope CN: Age-related effects of chlorpyrifos on acetylcholine release in rat brain. . Neurotoxicology. 2001 Feb;22(1):39-48.

Chlorpyrifos (CPF) is an organophosphorus insecticide that elicits toxicity through inhibition of acetylcholinesterase (AChE).
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14704222 Fryer AD, Lein PJ, Howard AS, Yost BL, Beckles RA, Jett DA: Mechanisms of organophosphate insecticide-induced airway hyperreactivity. . Am J Physiol Lung Cell Mol Physiol. 2004 May;286(5):L963-9. Epub 2004 Jan 2.

Mechanisms by which chlorpyrifos may cause airway hyperreactivity include inhibition of acetylcholinesterase (AChE) or dysfunction of M3 muscarinic receptors on airway smooth muscle or of autoinhibitory M2 muscarinic receptors on parasympathetic nerves in the lung.
82(1,1,1,2) Details
9585096 Mortensen SR, Hooper MJ, Padilla S: Rat brain acetylcholinesterase activity: developmental profile and maturational sensitivity to carbamate and organophosphorus inhibitors. Toxicology. 1998 Jan 16;125(1):13-9.

IC50s (the concentration of compound that inhibits 50% of the AChE activity in 30 min at 26 degrees C) defined concomitantly for postnatal day 4 and adult brain AChE using either aldicarb, carbaryl, chlorpyrifos-oxon or malaoxon were virtually identical at both ages with average IC50 values being: aldicarb = 2.4 microM, carbaryl = 1.7 microM, chlorpyrifos-oxon = 4.9 nM and malaoxon = 140 nM.
34(0,1,1,4) Details
12791540 Kropp TJ, Richardson RJ: Relative inhibitory potencies of chlorpyrifos oxon, chlorpyrifos methyl oxon, and mipafox for acetylcholinesterase versus neuropathy target esterase. J Toxicol Environ Health A. 2003 Jun 27;66(12):1145-57.
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11239688 Karen DJ, Klaine SJ, Ross PE: Further considerations of the skeletal system as a biomarker of episodic chlorpyrifos exposure. Aquat Toxicol. 2001 May;52(3-4):285-96.

Four daily or weekly 6 h exposures (2.5, 5.0, and 10.0 microg/l chlorpyrifos) in decreased salinity seawater (5 g/kg) significantly reduced brain AChE activity.
169(2,2,3,4) Details
9744565 Amitai G, Moorad D, Adani R, Doctor BP: Inhibition of acetylcholinesterase and butyrylcholinesterase by chlorpyrifos-oxon. Biochem Pharmacol. 1998 Aug 1;56(3):293-9.
168(2,2,2,8) Details
18254274 Musilek K, Kuca K, Jun D: Evaluation of potency of known oximes (pralidoxime, trimedoxime, HI-6, methoxime, obidoxime) to in vitro reactivate acetylcholinesterase inhibited by pesticides (chlorpyrifos and methylchlorpyrifos) and nerve agent (Russian VX). Acta Medica (Hradec Kralove). 2007;50(3):203-6.
166(2,2,2,6) Details
7531776 Chanda SM, Harp P, Liu J, Pope CN: Comparative developmental and maternal neurotoxicity following acute gestational exposure to chlorpyrifos in rats. J Toxicol Environ Health. 1995 Feb;44(2):189-202.

Chlorpyrifos (CPF), an organophosphorus (OP) insecticide, exerts toxicity through inhibition of acetylcholinesterase (AChE).
165(2,2,2,5) Details
11548114 Sanchez-Amate MC, Flores P, Sanchez-Santed F: Effects of chlorpyrifos in the plus-maze model of anxiety. Behav Pharmacol. 2001 Jul;12(4):285-92.

The purpose of the present study was to determine the effect of two different doses of the organophosphate insecticide O,O'-diethyl-O-3,5,6-trichloro-2-pyridylphosphorothionate [chlorpyrifos (CPF)], a cholinesterase (ChE) inhibitor, in the plus-maze test of anxiety in the rat, as well as on acetylcholinesterase (AChE) activity in the brain.
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12194025 Jeanty G, Wojciechowska A, Marty JL, Trojanowicz M: Flow-injection amperometric determination of pesticides on the basis of their inhibition of immobilized acetylcholinesterases of different origin. Anal Bioanal Chem. 2002 Apr;373(8):691-5. Epub 2002 Jun 12.

Determination of the organophosphorus pesticides paraoxon, chlorpyrifos oxon, and malaoxon has been performed by a method based on inhibition of acetylcholinesterase (AChE) and amperometric detection in a flow-injection system with enzymes obtained from the electric eel (eeAChE) and Drosophila melanogaster (dmAChE) and immobilized on the surface of platinum electrode within a layer of poly (vinyl alcohol) bearing styrylpyridinium groups. dmAChE is more sensitive than eeAChE to inhibition by chlorpyrifos oxon and paraoxon.
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8937895 Liu J, Pope CN: Effects of chlorpyrifos on high-affinity choline uptake and [3H] hemicholinium-3 binding in rat brain. Fundam Appl Toxicol. 1996 Nov;34(1):84-90.

High, subcutaneous doses of the organophosphorus insecticide chlorpyrifos (CPF) in adult male rats can be well-tolerated despite extensive and persistent acetylcholinesterase (AChE) inhibition.
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18576221 Picco EJ, Fernandez HR, David DC, San Andres MI, Boggio JC, Rodriguez C: Use of cholinesterase activity in monitoring chlorpyrifos exposure of steer cattle after topical administration. J Environ Sci Health B. 2008 Jun;43(5):405-9.

The aim of this work was to study the pharmacokinetic behavior and the inhibitory effect of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activities of chlorpyrifos (CPF) in steer cattle after pour-on administration.
33(0,1,1,3) Details
16288867 Musilek K, Kuca K, Jun D, Dohnal V, Dolezal M: Synthesis of the novel series of bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against chlorpyrifos-inhibited acetylcholinesterase. Bioorg Med Chem Lett. 2006 Feb;16(3):622-7. Epub 2005 Nov 8.
164(2,2,2,4) Details
18423506 Sultatos LG, Kaushik R: Altered binding of thioflavin t to the peripheral anionic site of acetylcholinesterase after phosphorylation of the active site by chlorpyrifos oxon or dichlorvos. Toxicol Appl Pharmacol. 2008 Aug 1;230(3):390-6. Epub 2008 Mar 15.
164(2,2,2,4) Details
16335048 Musilek K, Kuca K, Jun D, Dohnal V, Dolezal M: Synthesis of a novel series of bispyridinium compounds bearing a xylene linker and evaluation of their reactivation activity against chlorpyrifos-inhibited acetylcholinesterase. J Enzyme Inhib Med Chem. 2005 Oct;20(5):409-15.
163(2,2,2,3) Details
10421480 Costa LG, Li WF, Richter RJ, Shih DM, Lusis A, Furlong CE: The role of paraoxonase (PON1) in the detoxication of organophosphates and its human polymorphism. Chem Biol Interact. 1999 May 14;119-120:429-38.

Under these conditions, the acute toxicity (assessed by the degree of acetylcholinesterase inhibition) of paraoxon and chlorpyrifos oxon is significantly decreased, compared to control animals.
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17365099 Gultekin F, Karakoyun I, Sutcu R, Savik E, Cesur G, Orhan H, Delibas N: Chlorpyrifos increases the levels of hippocampal NMDA receptor subunits NR2A and NR2B in juvenile and adult rats. Int J Neurosci. 2007 Jan;117(1):47-62.

Chlorpyrifos significantly inhibited the AChE activity in juvenile and adult rats (p < .05).
81(1,1,1,1) Details
11093242 Harold JA, Ottea JA: Characterization of esterases associated with profenofos resistance in the tobacco budworm, Heliothis virescens (F.). Arch Insect Biochem Physiol. 2000 Oct;45(2):47-59.

Finally, reduction in the activity or the sensitivity of acetylcholinesterase to inhibition by chlorpyrifos oxon was observed in laboratory-selected and field-collected larvae that expressed resistance to profenofos.
81(1,1,1,1) Details
12474960 Owen R, Buxton L, Sarkis S, Toaspern M, Knap A, Depledge M: An evaluation of hemolymph cholinesterase activities in the tropical scallop, Euvola (Pecten) ziczac, for the rapid assessment of pesticide exposure. Mar Pollut Bull. 2002 Oct;44(10):1010-7.

Acute in vivo experiments showed inhibition of hemolymph acetylcholinesterase activity at concentrations of the organophosphate insecticide chlorpyrifos of 0.1, 1 and 10 ng l (-1).
33(0,1,1,3) Details
19337507 Laetz CA, Baldwin DH, Collier TK, Hebert V, Stark JD, Scholz NL: The synergistic toxicity of pesticide mixtures: implications for risk assessment and the conservation of endangered Pacific salmon. Environ Health Perspect. 2009 Mar;117(3):348-53. Epub 2008 Nov 14.

METHODS: We measured brain AChE inhibition in juvenile coho salmon (Oncorhynchus kisutch) exposed to sublethal concentrations of the organophosphates diazinon, malathion, and chlorpyrifos, as well as the carbamates carbaryl and carbofuran.
33(0,1,1,3) Details
11814330 Liu J, Chakraborti T, Pope C: In vitro effects of organophosphorus anticholinesterases on muscarinic receptor-mediated inhibition of acetylcholine release in rat striatum. Toxicol Appl Pharmacol. 2002 Jan 15;178(2):102-8.

Concentration-dependent inhibition of AChE activity in striatal slices perfused with chlorpyrifos oxon (0.1, 1, and 10 microM) suggested AChE inhibition was responsible for oxon-mediated alterations in ACh release.
163(2,2,2,3) Details
11748873 Latuszynska J, Luty S, Raszewski G, Tokarska-Rodak M, Przebirowska D, Przylepa E, Haratym-Maj A: Neurotoxic effect of dermally-applied chlorpyrifos and cypermethrin in Wistar rats. Ann Agric Environ Med. 2001;8(2):163-70.

The aim of the study was to evaluate the neurotoxic effect of a dermally-applied mixture of chlorpyrifos and cypermethrin in rats based on cognitive function, activity of the blood cholinesterase and brain acetylcholinesterase, as well as histologic brain examination.
163(2,2,2,3) Details
1381386 Hatano R, Scott JG, Dennehy TJ: Enhanced activation is the mechanism of negative cross-resistance to Chlorpyrifos in the Dicofol-IR strain of Tetranychus urticae (Acari: Tetranychidae). J Econ Entomol. 1992 Aug;85(4):1088-91.

The acetylcholinesterase of both strains was equally sensitive to inhibition by chlorpyrifos oxon.
81(1,1,1,1) Details
11846640 Cochran RC: Appraisal of risks from nonoccupational exposure to chlorpyrifos. . Regul Toxicol Pharmacol. 2002 Feb;35(1):105-21.

Most nonoccupational illnesses resulting from entry into areas treated with chlorpyrifos likely stem from odor, rather than the ability of the organophosphate to inhibit AChE.
81(1,1,1,1) Details
15470232 Lein PJ, Fryer AD: Organophosphorus insecticides induce airway hyperreactivity by decreasing neuronal M2 muscarinic receptor function independent of acetylcholinesterase inhibition. Toxicol Sci. 2005 Jan;83(1):166-76. Epub 2004 Oct 6.

We previously demonstrated that the organophosphorus (OP) insecticide chlorpyrifos potentiates vagally induced bronchoconstriction independent of acetylcholinesterase (AChE) inhibition by decreasing the function of neuronal M2 muscarinic receptors that normally inhibit acetylcholine release from parasympathetic nerves supplying airway smooth muscle.
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18484351 Tarhoni MH, Lister T, Ray DE, Carter WG: Albumin binding as a potential biomarker of exposure to moderately low levels of organophosphorus pesticides. Biomarkers. 2008 Jun;13(4):343-63.

At pesticide exposures producing approximately 30% inhibition of AChE, rat plasma albumin binding in vitro by azamethiphos (oxon), chlorfenvinphos (oxon), chlorpyrifos-oxon, diazinon-oxon and malaoxon was reduced from controls by 9+/-1%, 67+/-2%, 56+/-2%, 54+/-2% and 8+/-1%, respectively.
32(0,1,1,2) Details
16753212 Chandrasekara LW, Pathiratne A: Body size-related differences in the inhibition of brain acetylcholinesterase activity in juvenile Nile tilapia (Oreochromis niloticus) by chlorpyrifos and carbosulfan. Ecotoxicol Environ Saf. 2007 May;67(1):109-19. Epub 2006 Jun 6.

Three size groups of fish (fry: 3-4 cm, fingerlings: 6-8 cm, sub-adults: 10-12 cm in total length) were exposed to a series of concentrations of chlorpyrifos (0.5-12 microg L (-1)) or carbosulfan (1-10 microg L (-1)), and concentration-response for inhibition and recovery of the AChE enzyme was evaluated in comparison to the controls at different time points, 2, 6, 10, and 14 d.
148(1,3,3,8) Details
15141101 Kousba AA, Sultatos LG, Poet TS, Timchalk C: Comparison of chlorpyrifos-oxon and paraoxon acetylcholinesterase inhibition dynamics: potential role of a peripheral binding site. Toxicol Sci. 2004 Aug;80(2):239-48. Epub 2004 May 12.

The primary mechanism of action for organophosphorus (OP) insecticides, like chlorpyrifos and parathion, is to inhibit acetylcholinesterase (AChE) by their oxygenated metabolites (oxons), due to the phosphorylation of the serine hydroxyl group located in the active site of the molecule.
147(1,3,3,7) Details
15910416 Smith EG, Gordon CJ: The effects of chlorpyrifos on blood pressure and temperature regulation in spontaneously hypertensive rats. Basic Clin Pharmacol Toxicol. 2005 Jun;96(6):503-11.

Chlorpyrifos inhibits acetylcholinesterase activity, resulting in central and peripheral stimulation of central cholinergic pathways involved in blood pressure regulation.
81(1,1,1,1) Details
9469857 Moore MT, Huggett DB, Gillespie WB Jr, Rodgers JH Jr, Cooper CM: Comparative Toxicity of Chlordane, Chlorpyrifos, and Aldicarb to Four Aquatic Testing Organisms. Arch Environ Contam Toxicol. 1998 Feb;34(2):152-7.

Aqueous 48-h toxicity tests were performed to contrast responses of Daphnia magna Straus, Hyalella azteca Saussure, Chironomus tentans Fabricius, and Pimephales promelas Rafinesque to acetylcholinesterase-inhibiting insecticides: chlorpyrifos, aldicarb, and chlordane.
81(1,1,1,1) Details
8593081 Swann JM, Schultz TW, Kennedy JR: The effects of the organophosphorous insecticides Dursban and Lorsban on the ciliated epithelium of the frog palate in vitro. Arch Environ Contam Toxicol. 1996 Feb;30(2):188-94.

Since chlorpyrifos inhibits acetylcholinesterase, the acetylcholine-innervated ciliated epithelial cultures of frog palate were used as the model.
81(1,1,1,1) Details
17364862 Kuca K, Jun D, Bajgar J: Currently used cholinesterase reactivators against nerve agent intoxication: comparison of their effectivity in vitro. Drug Chem Toxicol. 2007;30(1):31-40.

In vitro comparison of reactivation efficacy of five currently used oximes - pralidoxime, obidoxime, trimedoxime, methoxime, and HI-6 (at two concentrations: 10-5 and 10-3 M) - against acetylcholinesterase (AChE; E.C. 3.1.1.7) inhibited by six different nerve agents (VX, Russian VX, sarin, cyclosarin, tabun, soman) and organophosphorus insecticide chlorpyrifos was the aim of this study.
32(0,1,1,2) Details
11223004 Timofeeva OA, Gordon CJ: Changes in EEG power spectra and behavioral states in rats exposed to the acetylcholinesterase inhibitor chlorpyrifos and muscarinic agonist oxotremorine. Brain Res. 2001 Mar 2;893(1-2):165-77.
32(0,1,1,2) Details
12175464 Timofeeva OA, Gordon CJ: EEG spectra, behavioral states and motor activity in rats exposed to acetylcholinesterase inhibitor chlorpyrifos. Pharmacol Biochem Behav. 2002 Jun;72(3):669-79.
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18164878 Moreno M, Canadas F, Cardona D, Sunol C, Campa L, Sanchez-Amate MC, Flores P, Sanchez-Santed F: Long-term monoamine changes in the striatum and nucleus accumbens after acute chlorpyrifos exposure. Toxicol Lett. 2008 Jan 30;176(2):162-7. Epub 2007 Nov 21.

This study examined the time-course effects (2, 7, 14 and 30 days) of acute chlorpyrifos (CPF) intoxication (250 mg/kg, s.c.) on monoamine systems and acetylcholinesterase (AChE) activity in the striatum and nucleus accumbens of adult male rats.
8(0,0,1,3) Details
19559912 Istamboulie G, Cortina-Puig M, Marty JL, Noguer T: The use of Artificial Neural Networks for the selective detection of two organophosphate insecticides: chlorpyrifos and chlorfenvinfos. Talanta. 2009 Jul 15;79(2):507-11. Epub 2009 Apr 16.

Amperometric acetylcholinesterase (AChE) biosensors have been developed to resolve mixtures of chlorpyrifos oxon (CPO) and chlorfenvinfos (CFV) pesticides.
7(0,0,1,2) Details
20027669 Musilek K, Dolezal M, Gunn-Moore F, Kuca K: Design, evaluation and structure-Activity relationship studies of the AChE reactivators against organophosphorus pesticides. Med Res Rev. 2009 Dec 21.

Organophosphate pesticides (OPPs; e.g. chlorpyrifos, diazinon, paraoxon) are a wide and heterogeneous group of organophosphorus compounds.
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16007003 Cole TB, Walter BJ, Shih DM, Tward AD, Lusis AJ, Timchalk C, Richter RJ, Costa LG, Furlong CE: Toxicity of chlorpyrifos and chlorpyrifos oxon in a transgenic mouse model of the human paraoxonase (PON1) Q192R polymorphism. Pharmacogenet Genomics. 2005 Aug;15(8):589-98.

Morbidity and acetylcholinesterase (AChE) activity in the brain and diaphragm were determined in the first 24 h following exposure.
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19564902 Eddleston M, Eyer P, Worek F, Juszczak E, Alder N, Mohamed F, Senarathna L, Hittarage A, Azher S, Jeganathan K, Jayamanne S, von Meyer L, Dawson AH, Sheriff MH, Buckley NA: Pralidoxime in acute organophosphorus insecticide poisoning--a randomised controlled trial. PLoS Med. 2009 Jun 30;6(6):e1000104. Epub 2009 Jun 30.

To reduce confounding due to ingestion of different insecticides, we further analysed patients with confirmed chlorpyrifos or dimethoate poisoning alone, finding no evidence of benefit.
Pralidoxime produced substantial and moderate red cell acetylcholinesterase reactivation in patients poisoned by diethyl and dimethyl compounds, respectively.
2(0,0,0,2) Details
15840715 Nomura DK, Leung D, Chiang KP, Quistad GB, Cravatt BF, Casida JE: A brain detoxifying enzyme for organophosphorus nerve poisons. Proc Natl Acad Sci U S A. 2005 Apr 26;102(17):6195-200. Epub 2005 Apr 19.

Organophosphorus (OP) insecticides and chemical warfare agents act primarily by inhibiting acetylcholinesterase.
There are many secondary targets for OP toxicants as observed for example with the major insecticide chlorpyrifos and its bioactivated metabolite chlorpyrifos oxon (CPO).
1(0,0,0,1) Details
19850121 Farag AT, Radwan AH, Sorour F, El Okazy A, El-Agamy el-S, El-Sebae Ael-K: Chlorpyrifos induced reproductive toxicity in male mice. Reprod Toxicol. 2010 Jan;29(1):80-5. Epub 2009 Oct 20.

Brain and skeletal muscle acetylcholinesterase activity was inhibited in the same groups.
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17324630 Corsi I, Pastore AM, Lodde A, Palmerini E, Castagnolo L, Focardi S: Potential role of cholinesterases in the invasive capacity of the freshwater bivalve, Anodonta woodiana (Bivalvia: Unionacea): a comparative study with the indigenous species of the genus, Anodonta sp. Comp Biochem Physiol C Toxicol Pharmacol. 2007 Apr;145(3):413-9. Epub 2007 Feb 1.

Calculated IC (50) for fenitrothion and chlorpyrifos was in the range 10 (-6)-10 (-3) M in muscle of A. woodiana while a higher inhibition was observed for fenitrothion (10 (-7) M) and lower for chlorpyrifos (10 (-2) M) in the indigenous species Anodonta sp.
The hypotheses of other authors that acetylcholinesterase (AChE) is involved in the control of many essential functions, such as frontal ciliary activity of gill epithelium, temperature resistance, ciliary activity for transport of suspended particulate, valve opening and embryo development, suggest that the high catalytic efficiency of the invasive species may endow it with a competitive advantage over the endemic species.
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12937891 Abou-Donia MB, Abdel-Rahman A, Goldstein LB, Dechkovskaia AM, Shah DU, Bullman SL, Khan WA: Sensorimotor deficits and increased brain nicotinic acetylcholine receptors following exposure to chlorpyrifos and/or nicotine in rats. Arch Toxicol. 2003 Aug;77(8):452-8. Epub 2003 Apr 26.

Biochemical analysis showed a decrease in cerebellar and an increase in midbrain acetylcholinesterase (AChE) activity following combined exposure.
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10773358 Gordon CJ, Padnos BK: Prolonged elevation in blood pressure in the unrestrained rat exposed to chlorpyrifos. Toxicology. 2000 Apr 20;146(1):1-13.

Organophosphate (OP) pesticides are likely to alter the regulation of blood pressure (BP) because (i) BP control centers in the brain stem utilize cholinergic synapses and (ii) the irreversible inhibition of acetylcholinesterase activity by OP's causes cholinergic stimulation in the CNS.
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7507502 Hemingway J, Small GJ, Monro AG: Possible mechanisms of organophosphorus and carbamate insecticide resistance in German cockroaches (Dictyoptera: Blattelidae) from different geographical areas. J Econ Entomol. 1993 Dec;86(6):1623-30.

One strain from Dubai had an altered acetylcholinesterase-based mechanism that conferred broad-spectrum resistance to a range of organophosphates and carbamates.
The resistance status of 14 strains of Blattella germanica (L.) from four countries was determined for chlorpyrifos and propoxur compared with a standard reference susceptible strain.
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20142434 Jiang W, Duysen EG, Hansen H, Shlyakhtenko L, Schopfer LM, Lockridge O: Mice treated with chlorpyrifos or chlorpyrifos oxon have organophosphorylated tubulin in the brain and disrupted microtubule structures, suggesting a role for tubulin in neurotoxicity associated with exposure to organophosphorus agents. Toxicol Sci. 2010 Feb 8.

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11158719 Carr RL, Chambers HW, Guarisco JA, Richardson JR, Tang J, Chambers JE: Effects of repeated oral postnatal exposure to chlorpyrifos on open-field behavior in juvenile rats. Toxicol Sci. 2001 Feb;59(2):260-7.

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11350194 van Gemert M, Dourson M, Moretto A, Watson M: Use of human data for the derivation of a reference dose for chlorpyrifos. . Regul Toxicol Pharmacol. 2001 Apr;33(2):110-6.

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10794393 Jett DA, Navoa RV: In vitro and in vivo effects of chlorpyrifos on glutathione peroxidase and catalase in developing rat brain. Neurotoxicology. 2000 Feb-Apr;21(1-2):141-5.

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15178118 Eder KJ, Leutenegger CM, Wilson BW, Werner I: Molecular and cellular biomarker responses to pesticide exposure in juvenile chinook salmon (Oncorhynchus tshawytscha). Mar Environ Res. 2004 Aug-Dec;58(2-5):809-13.

Significant differences in stress protein expression, cytokine transcription and AChE activity were found between control and surviving chlorpyrifos-exposed fish.
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17705656 Nillos MG, Rodriguez-Fuentes G, Gan J, Schlenk D: Enantioselective acetylcholinesterase inhibition of the organophosphorous insecticides profenofos, fonofos, and crotoxyphos. Environ Toxicol Chem. 2007 Sep;26(9):1949-54.

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9265078 Mortensen SR, Chanda SM, Hooper MJ, Padilla S: Maturational differences in chlorpyrifos-oxonase activity may contribute to age-related sensitivity to chlorpyrifos. J Biochem Toxicol. 1996;11(6):279-87.

This was accomplished by comparing the shifts in the tissue acetylcholinesterase (AChE) IC50 for CPFO in the presence or absence of CPFOase activity.
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11534899 Belden JB, Lydy MJ: Effects of atrazine on acetylcholinesterase activity in midges (Chironomus tentans) exposed to organophosphorus insecticides. Chemosphere. 2001 Sep;44(8):1685-9.

Although atrazine by itself did not reduce the level of acetylcholinesterase activity, atrazine in combination with chlorpyrifos significantly decreased acetylcholinesterase activity as compared to chlorpyrifos only treatments.
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17915512 Djogbenou L, Weill M, Hougard JM, Raymond M, Akogbeto M, Chandre F: Characterization of insensitive acetylcholinesterase (ace-1R) in Anopheles gambiae (Diptera: Culicidae): resistance levels and dominance. J Med Entomol. 2007 Sep;44(5):805-10.

Furthermore, the dominance status varied between semi-recessivity with fenitrothion and chlorpyrifos methyl insecticides to semidominance with temephos, carbosulfan, and propoxur.
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11425027 Lee SE, Lees EM: Biochemical mechanisms of resistance in strains of Oryzaephilus surinamensis (Coleoptera: Silvanidae) resistant to malathion and chlorpyrifos-methyl. J Econ Entomol. 2001 Jun;94(3):706-13.

The acetylcholinesterase, carboxylesterase, and cytochrome P450 monooxygenase activities of three strains of Oryzaephilus srinamensis (L.) were examined to better understand biochemical mechanisms of resistance.
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15772369 Canadas F, Cardona D, Davila E, Sanchez-Santed F: Long-term neurotoxicity of chlorpyrifos: spatial learning impairment on repeated acquisition in a water maze. Toxicol Sci. 2005 Jun;85(2):944-51. Epub 2005 Mar 16.

Their major mechanism of acute toxic action is the inhibition of acetylcholinesterase, which is responsible for the degradation of the neurotransmitter acetylcholine.
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15557345 Buratti FM, D'Aniello A, Volpe MT, Meneguz A, Testai E: Malathion bioactivation in the human liver: the contribution of different cytochrome p450 isoforms. Drug Metab Dispos. 2005 Mar;33(3):295-302. Epub 2004 Nov 22.

These results are in line with those found with chlorpyrifos, diazinon, azynphos-methyl, and parathion, characterized by the presence of an aromatic ring in the molecule.
Malathion desulfuration has been characterized in human liver microsomes (HLMs) with a method based on acetylcholinesterase inhibition that is able to detect nanomolar levels of oxon.
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15719990 Osten JR, Soares AM, Guilhermino L: Black-bellied whistling duck (Dendrocygna autumnalis) brain cholinesterase characterization and diagnosis of anticholinesterase pesticide exposure in wild populations from Mexico. Environ Toxicol Chem. 2005 Feb;24(2):313-7.

The pesticides used to control pests of this crop mainly are carbofuran, chlorpyrifos, and glyphosate.
We found that acetylcholinesterase (AChE) seems to be the predominant ChE form in the biological fraction analyzed.
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11459102 Pogacnik L, Franko M: Determination of organophosphate and carbamate pesticides in spiked samples of tap water and fruit juices by a biosensor with photothermal detection. Biosens Bioelectron. 1999 Jun 30;14(6):569-78.

The determination of organophosphate (paraoxon, chlorpyrifos, diazinon) and carbamate (carbaryl, carbofuran) pesticides in spiked drinking water and fruit juices was carried out using a photothermal biosensor.
The biosensor consists of a cartridge containing immobilised enzyme acetylcholinesterase (AChE) placed in a flow-injection analysis (FIA) manifold and a photothermal detector based on thermal lens spectrometry.
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16783542 Laviola G, Adriani W, Gaudino C, Marino R, Keller F: Paradoxical effects of prenatal acetylcholinesterase blockade on neuro-behavioral development and drug-induced stereotypies in reeler mutant mice. Psychopharmacology. 2006 Aug;187(3):331-44. Epub 2006 Jun 17.

Chlorpyrifos, a potent and reversible acetylcholinesterase blocker used as a pesticide, and the "reeler" mouse, lacking the extracellular-matrix protein Reelin, were used.
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8801577 Chanda SM, Pope CN: Neurochemical and neurobehavioral effects of repeated gestational exposure to chlorpyrifos in maternal and developing rats. Pharmacol Biochem Behav. 1996 Apr;53(4):771-6.

Extensive acetylcholinesterase (AChE) inhibition (83-90%) was noted in maternal brain at all three time points following repeated exposures (25 mg/kg).
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11861971 Timchalk C, Nolan RJ, Mendrala AL, Dittenber DA, Brzak KA, Mattsson JL: A Physiologically based pharmacokinetic and pharmacodynamic (PBPK/PD) model for the organophosphate insecticide chlorpyrifos in rats and humans. Toxicol Sci. 2002 Mar;66(1):34-53.

The time course of CPF and TCP in both species was linear over the dose range evaluated, and the model reasonably simulated the dose-dependent inhibition of plasma ChE, RBC acetylcholinesterase (AChE), and brain (rat only) AChE.
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19061257 Mitra NK, Siong HH, Nadarajah VD: Evaluation of neurotoxicity of repeated dermal application of chlorpyrifos on hippocampus of adult mice. Ann Agric Environ Med. 2008 Dec;15(2):211-6.

AChE levels in the serum and brain were estimated using a spectrophotometric method (Amplex Red reagent).
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9615543 Ben Cheikh H, Ben Ali-Haouas Z, Marquine M, Pasteur N: Resistance to organophosphorus and pyrethroid insecticides in Culex pipiens (Diptera: Culicidae) from Tunisia. J Med Entomol. 1998 May;35(3):251-60.

Resistance to the organophosphates temephos and chlorpyrifos, the carbamate propoxur, the pyrethroid permethrin, and the organochloride DDT was investigated in Tunisian populations of Culex pipiens pipiens (L.) collected between 1990 and 1996.
To better understand the factors influencing the distribution of resistance in Tunisia, the polymorphism of genes involved in organophosphate resistance (i.e., over-produced esterases and insensitive acetylcholinesterase) was investigated in relation to the genetic structure of populations studied by analyzing the electrophoretic polymorphism of "neutral" genes.
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15620756 Rendon-von Osten J, Ortiz-Arana A, Guilhermino L, Soares AM: In vivo evaluation of three biomarkers in the mosquitofish (Gambusia yucatana) exposed to pesticides. Chemosphere. 2005 Feb;58(5):627-36.

In this study, the acute toxicity and the in vivo effects of commercial chlorpyrifos, carbofuran and glyphosate formulations on cholinesterase (ChE), glutathione S-transferase (GST) and lactate dehydrogenase (LDH) activities of the mosquitofish (Gambusia yucatana) were investigated.
The results obtained suggest that the enzyme present in both head and muscle of G. yucatana is mainly acetylcholinesterase (AChE).
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8571366 Chambers JE, Carr RL: Biochemical mechanisms contributing to species differences in insecticidal toxicity. Toxicology. 1995 Dec 28;105(2-3):291-304.


However, in the channel catfish, the acetylcholinesterase sensitivity to oxon inhibition reflects the acute toxicity level of these same insecticides, and may be largely responsible for determining the acute toxicity level in this species.
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18384877 Leticia AG, Gerardo GB: Determination of esterase activity and characterization of cholinesterases in the reef fish Haemulon plumieri. Ecotoxicol Environ Saf. 2008 Mar 31.

Furthermore, ChEs detected in brain, liver and muscle were characterized, and results suggested that the acetylcholinesterase (AChE) type was more abundant relative to pseudocholinesterase (BChE) which was rare.
Finally, an additional experiment in vitro showed a significant decrease in both ChE and CbE activities when different tissues were exposed to model xenobiotics, such as benzo [a] pyrene and Chlorpyrifos.
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15154489 Grafton-Cardwell EE, Ouyang Y, Striggow RA, Christiansen JA, Black CS: Role of esterase enzymes in monitoring for resistance of California red scale, Aonidiella aurantii (Homoptera: Diaspididae), to organophosphate and carbamate insecticides. J Econ Entomol. 2004 Apr;97(2):606-13.

Eighty-seven populations of California red scale, Aonidiella aurantii (Maskell), from the San Joaquin Valley of California were tested for insecticide resistance by using chlorpyrifos, methidathion, and/or carbaryl in a standard fruit-dip bioassay as well as for general esterase activity by using alpha-naphthyl acetate as a substrate in a colorimetric test.
The results of tests for activity and inhibition of acetylcholinesterase activity suggest that California red scale is using increased amounts of esterase enzymes, including acetylcholinesterase, to sequester organophosphate and carbamate insecticides, rather than modified acetylcholinesterase.
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17079358 Foxenberg RJ, McGarrigle BP, Knaak JB, Kostyniak PJ, Olson JR: Human hepatic cytochrome p450-specific metabolism of parathion and chlorpyrifos. Drug Metab Dispos. 2007 Feb;35(2):189-93. Epub 2006 Nov 1.

Thiophosphorus OPs, once bioactivated by cytochromes P450 (P450s), form oxon metabolites, which are potent acetylcholinesterase inhibitors.
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11718958 Dyer SM, Cattani M, Pisaniello DL, Williams FM, Edwards JW: Peripheral cholinesterase inhibition by occupational chlorpyrifos exposure in Australian termiticide applicators. Toxicology. 2001 Dec 28;169(3):177-85.

Occupational exposure to organophosphorus insecticides (OPs), such as chlorpyrifos, may be monitored by the measurement of the activity of peripheral cholinesterase (ChE) enzymes, including erythrocyte acetylcholinesterase (EAChE) and serum cholinesterase (SChE).
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10686320 Lund SA, Fulton MH, Key PB: The sensitivity of grass shrimp, Palaemonetes pugio, embryos to organophosphate pesticide induced acetylcholinesterase inhibition. Aquat Toxicol. 2000 Mar 1;48(2-3):127-134.

Embryos were exposed for 24 h to either chlorpyrifos or malathion.
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17097717 Bavcon Kralj M, Franko M, Trebse P: Photodegradation of organophosphorus insecticides - investigations of products and their toxicity using gas chromatography-mass spectrometry and AChE-thermal lens spectrometric bioassay. Chemosphere. 2007 Feb;67(1):99-107. Epub 2006 Nov 13.

Four organophosphorus compounds: azinphos-methyl, chlorpyrifos, malathion and malaoxon in aqueous solution were degraded by using a 125 W xenon parabolic lamp.
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20087798 Cardona D, Lopez-Crespo G, Sanchez-Amate MC, Flores P, Sanchez-Santed F: Impulsivity as Long-Term Sequelae After Chlorpyrifos Intoxication: Time Course and Individual Differences. Neurotox Res. 2010 Jan 20.

The primary mechanism of acute toxic action of OPs is initiated by acetylcholinesterase (AChE) inhibition.
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11876500 Zhang H, Liu J, Pope CN: Age-related effects of chlorpyrifos on muscarinic receptor-mediated signaling in rat cortex. Arch Toxicol. 2002 Jan;75(11-12):676-84.

A number of studies suggest that in addition to inhibiting acetylcholinesterase (AChE), CPF oxon may also interact directly with m2 and/or m4 subtypes of muscarinic acetylcholine receptors (mAChRs).
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19894225 Khajehali J, Van Leeuwen T, Grispou M, Morou E, Alout H, Weill M, Tirry L, Vontas J, Tsagkarakou A: Acetylcholinesterase point mutations in European strains of Tetranychus urticae (Acari: Tetranychidae) resistant to organophosphates. Pest Manag Sci. 2010 Feb;66(2):220-8.

RESULTS: The resistance ratios of the OP strains varied from 9 to 43 for pirimiphos-methyl, from 78 to 586 for chlorpyrifos, from 8 to 333 for methomyl and from 137 to 4164 for dimethoate.
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16042503 Lotti M, Moretto A: Organophosphate-induced delayed polyneuropathy. . Toxicol Rev. 2005;24(1):37-49.

The ratio of inhibitory powers for acetylcholinesterase and NTE represents the crucial guideline for the aetiological attribution of OP-induced peripheral neuropathy.
In this article, we mainly discuss OP pesticide poisoning, particularly when caused by chlorpyrifos, dichlorvos, isofenphos, methamidophos, mipafox, trichlorfon, trichlornat, phosphamidon/mevinphos and by certain carbamates.
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15081274 Vidair CA: Age dependence of organophosphate and carbamate neurotoxicity in the postnatal rat: extrapolation to the human. Toxicol Appl Pharmacol. 2004 Apr 15;196(2):287-302.

Because these compounds probably exert their neurotoxic effects through the inhibition of acetylcholinesterase (AChE), the above question can be narrowed to whether the cholinesterase inhibition and neurotoxicity they produce is age-dependent, both in terms of the effects produced and potency.
Four pesticides were tested in rat pups in their third postnatal week: aldicarb, chlorpyrifos, malathion, and methamidophos.
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9344890 Katz EJ, Cortes VI, Eldefrawi ME, Eldefrawi AT: Chlorpyrifos, parathion, and their oxons bind to and desensitize a nicotinic acetylcholine receptor: relevance to their toxicities. Toxicol Appl Pharmacol. 1997 Oct;146(2):227-36.

The data suggest that in addition to inhibition of acetylcholinesterase, these OPs bind to a site on the nAChR that is different from the sites that bind ACh or TCP and that this binding induces nAChR desensitization.
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16966160 Binelli A, Ricciardi F, Riva C, Provini A: Integrated use of biomarkers and bioaccumulation data in Zebra mussel (Dreissena polymorpha) for site-specific quality assessment. Biomarkers. 2006 Sep-Oct;11(5):428-48.

In this study, several persistent organic pollutants -- 23 polychlorinated biphenyl (PCB) congeners, 11 polycyclic aromatic hydrocarbons (PAHs), six dichlorodiphenyltricholroethane (DDT) relatives, hexachlorobenzene (HCB), chlorpyrifos and its oxidized metabolite -- and some herbicides (lindane and the isomers alpha, beta, delta; terbutilazine; alachlor; metolachlor) were measured in the soft tissues of the freshwater mollusc Zebra mussel (Dreissena polymorpha) from 25 sampling sites in the Italian portions of the sub-alpine great lakes along with the measure of ethoxyresorufin dealkylation (EROD) and acetylcholinesterase (AChE) activity.
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11878473 Jin-Clark Y, Lydy MJ, Zhu KY: Effects of atrazine and cyanazine on chlorpyrifos toxicity in Chironomus tentans (Diptera: Chironomidae). Environ Toxicol Chem. 2002 Mar;21(3):598-603.

We observed a positive correlation between the degree of inhibition of AChE and the concentration of atrazine or cyanazine in the presence of a fixed concentration of chlorpyrifos.
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16510359 Pung T, Klein B, Blodgett D, Jortner B, Ehrich M: Examination of concurrent exposure to repeated stress and chlorpyrifos on cholinergic, glutamatergic, and monoamine neurotransmitter systems in rat forebrain regions. Int J Toxicol. 2006 Jan-Feb;25(1):65-80.

Effects of concurrent exposure to repeated stress and chlorpyrifos on activities of acetylcholinesterase (AChE), carboxylesterase, and choline acetyltransferase (ChAT); concentrations of excitatory amino acids, monoamines, and their metabolites; and maximum binding densities (B (max)) and equilibrium dissociation rate constants (K (d)) of glutamatergic N-methyl-d-aspartate (NMDA) and total muscarinic cholinergic receptors were studied in the blood, hippocampus, cerebral cortex, or hypothalamus of adult Long-Evans rats.
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7514668 Rivet Y, Raymond M, Rioux JA, Delalbre A, Pasteur N: Resistance monitoring in Culex pipiens (Diptera: Culicidae) from central-eastern France. J Med Entomol. 1994 Mar;31(2):231-9.

Insensitive acetylcholinesterase (AceR) and five over-produced esterases (A1, A2 and B2, and A4 and B4) involved in detoxification are responsible for resistance to organophosphorous insecticides (OPs) in Culex pipiens L. from the Rhone-Alpes region, where C. pipiens control is mainly accomplished with the OPs temephos and chlorpyrifos using 0.15 mg/liter doses.
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9880902 Gao JR, Rao JV, Wilde GE, Zhu KY: Purification and kinetic analysis of acetylcholinesterase from western corn rootworm, Diabrotica virgifera virgifera (Coleoptera: Chrysomelidae). Arch Insect Biochem Physiol. 1998;39(3):118-25.

Insecticides or their oxidative metabolites, chlorpyrifos-methyl oxon, carbofuran, carbaryl, malaoxon, and paraoxon, used in in vitro kinetic study exhibited high inhibition to AChE purified from WCR.
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15474619 Poet TS, Kousba AA, Dennison SL, Timchalk C: Physiologically based pharmacokinetic/pharmacodynamic model for the organophosphorus pesticide diazinon. Neurotoxicology. 2004 Dec;25(6):1013-30.

This model further confirms the usefulness of the model structure previously validated for chlorpyrifos and shows the potential utility of the model framework for other related organophosphate pesticides.
The toxicological effects of DZN are primarily mediated through the effects of its toxic metabolite, DZN-oxon on acetylcholinesterases, which results in accumulation of acetylcholine at neuronal junctions.
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10214458 Lakew K, Mekonnen Y: The health status of northern Omo State Farm workers exposed to chlorpyrifos and profenofos. Ethiop Med J. 1998 Jul;36(3):175-84.

Plasma ChE (PChE) and erythrocyte ChE (AChE) activities were determined electrometrically before and after pesticide exposure.
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19674799 Tryfonos M, Papaefthimiou C, Antonopoulou E, Theophilidis G: Comparing the inhibitory effects of five protoxicant organophosphates (azinphos-methyl, parathion-methyl, chlorpyriphos-methyl, methamidophos and diazinon) on the spontaneously beating auricle of Sparus aurata: an in vitro study. Aquat Toxicol. 2009 Sep 14;94(3):211-8. Epub 2009 Jul 16.


Organophosphates (OPs) can provoke toxicity by inhibiting acetylcholinesterase (AChE) in non-target organisms, like fish.
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8642625 Wilson BW, Padilla S, Henderson JD, Brimijoin S, Dass PD, Elliot G, Jaeger B, Lanz D, Pearson R, Spies R: Factors in standardizing automated cholinesterase assays. J Toxicol Environ Health. 1996 Jun 7;48(2):187-95.


The ChE activity in erythrocyte samples differed more between laboratories due to a high blank, low erythrocyte AChE activity and hemoglobin absorption at the wavelength of the assay.
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17549541 Venkateswara Rao J, Kavitha P, Jakka NM, Sridhar V, Usman PK: Toxicity of organophosphates on morphology and locomotor behavior in brine shrimp, Artemia salina. Arch Environ Contam Toxicol. 2007 Aug;53(2):227-32. Epub 2007 Jun 1.

The acute toxicity and hatching success of four organophosphorus insecticides--acephate (ACEP), chlorpyrifos (CPP), monocrotophos (MCP), and profenofos (PF)--was studied in a short-term bioassay using brine shrimp, Artemia salina.
The in vivo effect of these insecticides on acetylcholinesterase (Enzyme commission number (EC 3.1.1.7) activity was also determined in LC (50)-exposed nauplii after 24 hours.
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11484908 Smith EC, Padnos B, Cordon CJ: Peripheral versus central muscarinic effects on blood pressure, cardiac contractility, heart rate, and body temperature in the rat monitored by radiotelemetry. Pharmacol Toxicol. 2001 Jul;89(1):35-42.

Since organophosphate pesticides inhibit acetylcholinesterase activity and cause cholinergic stimulation in the central nervous system and peripheral tissues, we suspect that the hypertensive response from chlorpyrifos is elicited by activation of pressor areas in the brain stem, specifically muscarinic receptors which are known to mediate hypertensive responses.
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11835623 Olivier K Jr, Liu J, Pope C: Inhibition of forskolin-stimulated cAMP formation in vitro by paraoxon and chlorpyrifos oxon in cortical slices from neonatal, juvenile, and adult rats. J Biochem Mol Toxicol. 2001;15(5):263-9.

Parathion (PS) and chlorpyrifos (CPF) are organophosphorus insecticides, which elicit toxicity following biotransformation to the potent acetylcholinesterase inhibitors, paraoxon (PO) and chlorpyrifos oxon (CPO).
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17974266 Zhang YL, Mu W, Chen ZL, Han ZR, Ma C, Zhai RH: [Susceptibility and related physiological and biochemical mechanisms of Carposina niponensis Walsingham larvae on six insecticides before and after overwintering]. Ying Yong Sheng Tai Xue Bao. 2007 Aug;18(8):1913-6.

The study with impregnating method showed that after overwintering, the susceptibility of Carposina niponensis larvae on triazophos, phoxim, chlorpyrifos, malathion, lambda-cyhalothrin and abamectin was 34.50, 16.71, 3.89, 3.28, 5.90 and 2.73 times as much as that before overwintering, the total protein, glycogen and fat contents and carboxylesterase, acid phosphatase, alkaline phosphatase, glutathione-S-transferase, superoxide dismutase, catalase and peroxidase activities in C. niponensis larvae were decreased by 17.10%, 41.76% and 30.08%, 62.36%, 53.47%, 76.19%, 80.60%, 18.77%, 14.16% and 64.02%, respectively, and the activity of acetylcholinesterase, the target enzyme of many insecticides, was 1.41 times as much as that before overwintering.
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18668222 Stapleton AR, Chan VT: Subtoxic chlorpyrifos treatment resulted in differential expression of genes implicated in neurological functions and development. Arch Toxicol. 2009 Apr;83(4):319-33. Epub 2008 Jul 31.

Chlorpyrifos (CPF), a commonly used organophosphorus insecticide, induces acetylcholinesterase inhibition and cholinergic toxicity.
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17418885 Sturm A, Radau TS, Hahn T, Schulz R: Inhibition of rainbow trout acetylcholinesterase by aqueous and suspended particle-associated organophosphorous insecticides. Chemosphere. 2007 Jun;68(4):605-12. Epub 2007 Apr 6.

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17129656 Amitai G, Adani R, Yacov G, Yishay S, Teitlboim S, Tveria L, Limanovich O, Kushnir M, Meshulam H: Asymmetric fluorogenic organophosphates for the development of active organophosphate hydrolases with reversed stereoselectivity. Toxicology. 2007 Apr 20;233(1-3):187-98. Epub 2006 Oct 13.

We have previously identified three key positions in PON1 that affect OP hydrolysis: Leu69, Val346 and His115, that significantly enhance the hydrolysis of cyclosarin (GF), soman, chlorpyrifos-oxon (ChPo), O-isopropyl-O-(p-nitrophenyl) methylphosphonate (IMP-pNP) and diisopropyl fluorophosphate (DFP).
GC/FPD analysis compared to residual AChE inhibition assay displayed stereoselective hydrolysis of GF, soman and IMP-pNP, indicating that wild type PON1 and its variant V346A are more active toward the less toxic P (+) optical isomer.
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19130375 Somerset V, Baker P, Iwuoha E: Mercaptobenzothiazole-on-gold organic phase biosensor systems: 1. J Environ Sci Health B. 2009 Feb;44(2):164-78.

This paper reports the construction of the gold/mercaptobenzothiazole/polyaniline/acetylcholinesterase/polyvinylaceta te (Au/ MBT/PANI/AChE/PVAc) thick-film biosensor for the determination of certain organophosphate pesticide solutions in selected aqueous organic solvent solutions.
The biosensor was then applied to detect a series of 5 organophosphorous pesticides in aqueous organic solvents and the pesticides studied were parathion-methyl, malathion and chlorpyrifos.
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7688795 Severini C, Romi R, Marinucci M, Raymond M: Mechanisms of insecticide resistance in field populations of Culex pipiens from Italy. J Am Mosq Control Assoc. 1993 Jun;9(2):164-8.


The A1, A4-B4 and/or A5-B5 nonspecific esterases and insensitive acetylcholinesterase (AChE) were detected in our samples.
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16872049 Singh M, Sandhir R, Kiran R: Erythrocyte antioxidant enzymes in toxicological evaluation of commonly used organophosphate pesticides. Indian J Exp Biol. 2006 Jul;44(7):580-3.

Present work is designed to study the in vitro effects of some organophosphates (ethion, chlorpyrifos, dimethoate and monocrotophos) on rat erythrocytes.
Membrane bound enzymes like acetylcholinesterase (AChE), Na (+)-K (+)-ATPase and Ca (2+)-ATPase were also inhibited.
1(0,0,0,1) Details
15560889 Usmani KA, Hodgson E, Rose RL: In vitro metabolism of carbofuran by human, mouse, and rat cytochrome P450 and interactions with chlorpyrifos, testosterone, and estradiol. Chem Biol Interact. 2004 Dec 7;150(3):221-32.

Its effect as a pesticide is due to its ability to inhibit acetylcholinesterase activity.
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11205075 Guadarrama-Naveda M, de Cabrera LC, Matos-Bastidas S: Intermediate syndrome secondary to ingestion of chlorpiriphos. Vet Hum Toxicol. 2001 Feb;43(1):34.


These clinical manifestations occur from liposoluble organophosphates or metabolites with long-lasting half time, causeing delayed inhibition of acetylcholinesterase and subsequent burn out of the neuromuscular junction from acetylcholine overstimulation.
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7509414 Chaudhuri J, Chakraborti TK, Chanda S, Pope CN: Differential modulation of organophosphate-sensitive muscarinic receptors in rat brain by parathion and chlorpyrifos. J Biochem Toxicol. 1993 Dec;8(4):207-16.

Because extensive acetylcholinesterase inhibition often induces compensatory changes in cholinergic receptor populations, we compared the effects of parathion and chlorpyrifos on brain muscarinic receptors.
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15451035 Levin ED, Swain HA, Donerly S, Linney E: Developmental chlorpyrifos effects on hatchling zebrafish swimming behavior. Neurotoxicol Teratol. 2004 Nov-Dec;26(6):719-23.

Chlorpyrifos (CPF), a widely used organophosphate insecticide and potent acetylcholinesterase inhibitor, interferes with neurobehavioral development.
31(0,1,1,1) Details
19900550 Revuelta L, Piulachs MD, Belles X, Castanera P, Ortego F, Diaz-Ruiz JR, Hernandez-Crespo P, Tenllado F: RNAi of ace1 and ace2 in Blattella germanica reveals their differential contribution to acetylcholinesterase activity and sensitivity to insecticides. Insect Biochem Mol Biol. 2009 Dec;39(12):913-9. Epub 2009 Nov 10.

A significant increase in sensitivity of Bgace1-interfered cockroaches was observed after 48 h of exposure to chlorpyrifos.
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12207238 Andreescu S, Avramescu A, Bala C, Magearu V, Marty JL: Detection of organophosphorus insecticides with immobilized acetylcholinesterase - comparative study of two enzyme sensors. Anal Bioanal Chem. 2002 Sep;374(1):39-45. Epub 2002 Jul 30.

Screen-printed sensors were used to detect the organophosphorus pesticides paraoxon and chlorpyrifos ethyl oxon; the detection limits achieved with phenyl acetate as substrate were 5.2x10 (-3) mg L (-1) and 0.56x10 (-3) mg L (-1), respectively.
4(0,0,0,4) Details
17571690 Eder KJ, Kohler HR, Werner I: Pesticide and pathogen: heat shock protein expression and acetylcholinesterase inhibition in juvenile Chinook salmon in response to multiple stressors. Environ Toxicol Chem. 2007 Jun;26(6):1233-42.

Both pesticides, EV and the organophosphate (OP) chlorpyrifos (CP), as well as virus exposure, induced hsp expression, but highest hsp levels were observed after the combined treatments, suggesting an additive effect between virus and pesticides.
4(0,0,0,4) Details
16962835 Poyot T, Nachon F, Froment MT, Loiodice M, Wieseler S, Schopfer LM, Lockridge O, Masson P: Mutant of Bungarus fasciatus acetylcholinesterase with low affinity and low hydrolase activity toward organophosphorus esters. Biochim Biophys Acta. 2006 Sep;1764(9):1470-8. Epub 2006 Aug 4.

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18577432 Farid AS, Horii Y: Gastrointestinal nematode infection increases organophosphate toxicity in rats. Toxicol Lett. 2008 Jul 30;180(1):33-7. Epub 2008 Jun 3.

In the present study we investigated the effects of decreased serum PON1 activity due to N. brasiliensis infection on acute toxicity induced by chlorpyrifos oxon (CPO) and paraoxon (PO) in rats.
CPO and PO were dermally applied at doses of 8 mg/kg and 0.2 mg/kg body weight, respectively, to infected (on day 7 post-infection) and uninfected rats, after which acetylcholinesterase (AChE) activity was measured within the brain, diaphragm, plasma, and red blood cells, 4h after administration as a measure of toxicity.
2(0,0,0,2) Details
18096363 Timofeeva OA, Roegge CS, Seidler FJ, Slotkin TA, Levin ED: Persistent cognitive alterations in rats after early postnatal exposure to low doses of the organophosphate pesticide, diazinon. Neurotoxicol Teratol. 2008 Jan-Feb;30(1):38-45. Epub 2007 Oct 24.

The addition of some inhibition of AChE with a higher dose reversed the cognitive impairment.
We have found persisting effects of developmental chlorpyrifos (CPF) and diazinon (DZN) on cholinergic and serotonergic neurotransmitter systems and gene expression as well as behavioral function.
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20096330 Rush T, Liu XQ, Hjelmhaug J, Lobner D: Mechanisms of chlorpyrifos and diazinon induced neurotoxicity in cortical culture. Neuroscience. 2010 Mar 31;166(3):899-906. Epub 2010 Jan 20.

The main action of organophosphorous insecticides is generally believed to be the inhibition of acetylcholinesterase (AChE).
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9439736 Atterberry TT, Burnett WT, Chambers JE: Age-related differences in parathion and chlorpyrifos toxicity in male rats: target and nontarget esterase sensitivity and cytochrome P450-mediated metabolism. Toxicol Appl Pharmacol. 1997 Dec;147(2):411-8.

Developmental changes in brain acetylcholinesterase and hepatic aliesterase (carboxylesterase), cytochrome P450, and the P450-mediated metabolism of these two phosphorothionate insecticides were investigated in male Sprague-Dawley rats.
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8846108 Ward TR, Mundy WR: Organophosphorus compounds preferentially affect second messenger systems coupled to M2/M4 receptors in rat frontal cortex. Brain Res Bull. 1996;39(1):49-55.

Recent reports indicate that organophosphate insecticides, in addition to inhibiting acetylcholinesterase activity, can bind directly at a subset of muscarinic receptors, which also bind cis-methyldioxolane with high affinity.
We have investigated the action of the active forms of parathion, malathion, and chlorpyrifos (paraoxon, malaoxon, and chlorpyrifos oxon, respectively) on these second messenger systems in cortical slices from adult male Long-Evans rats.
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15019964 Sanchez-Santed F, Canadas F, Flores P, Lopez-Grancha M, Cardona D: Long-term functional neurotoxicity of paraoxon and chlorpyrifos: behavioural and pharmacological evidence. Neurotoxicol Teratol. 2004 Mar-Apr;26(2):305-17.

The major mechanism of acute toxic action is the inhibition of acetylcholinesterase (AChE), which is responsible for the degradation of the neurotransmitter acetylcholine.
1(0,0,0,1) Details
9788582 Li W, Casida JE: Organophosphorus neuropathy target esterase inhibitors selectively block outgrowth of neurite-like and cell processes in cultured cells. Toxicol Lett. 1998 Sep 15;98(3):139-46.

This study compares two direct-acting neuropathy target esterase (NTE) inhibitors (mipafox and 2-octyl-4H-1,3,2-benzodioxophosphorin 2-oxide (OBDPO)), a metabolic precursor to an NTE inhibitor (tri-o-cresyl phosphate or TOCP) and a potent acetylcholinesterase inhibitor (chlorpyrifos oxon or CPO) for their effects on outgrowth of neurite-like and cell processes and on viability in differentiated cultured cells (rat adrenal pheochromocytoma (PC-12) and brain glial tumor (C6)).
31(0,1,1,1) Details
14555401 Abdel-Rahman A, Dechkovskaia A, Mehta-Simmons H, Guan X, Khan W, Abou-Donia M: Increased expression of glial fibrillary acidic protein in cerebellum and hippocampus: differential effects on neonatal brain regional acetylcholinesterase following maternal exposure to combined chlorpyrifos and nicotine. J Toxicol Environ Health A. 2003 Nov 14;66(21):2047-66.
25(0,0,4,5) Details
16482470 Abou-Donia MB, Khan WA, Dechkovskaia AM, Goldstein LB, Bullman SL, Abdel-Rahman A: In utero exposure to nicotine and chlorpyrifos alone, and in combination produces persistent sensorimotor deficits and Purkinje neuron loss in the cerebellum of adult offspring rats. Arch Toxicol. 2006 Sep;80(9):620-31. Epub 2006 Feb 16.

Brainstem and cerebellum of female offspring from mothers treated with nicotine or chlorpyrifos, alone or in combination showed increased AChE activity, whereas brainstem of male offspring from mothers treated with nicotine alone or a combination of nicotine and chlorpyrifos showed increase in AChE activity.
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10025366 Gomes J, Dawodu AH, Lloyd O, Revitt DM, Anilal SV: Hepatic injury and disturbed amino acid metabolism in mice following prolonged exposure to organophosphorus pesticides. Hum Exp Toxicol. 1999 Jan;18(1):33-7.

Chronic occupational exposure to organophosphorus and carbamate-type pesticides significantly inhibits acetylcholinesterase activity and causes morbidity.
Laboratory mice were exposed to a formulated mixture of the six organophosphorus pesticides (Dimethoate, Chlorpyrifos, Profenofos, Pirimiphos methyl, Triazophos and Dimethoate) most commonly used in agriculture in this region of the Middle East.
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16263378 Binelli A, Ricciardi F, Riva C, Provini A: Screening of POP pollution by AChE and EROD activities in Zebra mussels from the Italian Great Lakes. Chemosphere. 2005 Dec;61(8):1074-82. Epub 2005 Apr 25.

4(0,0,0,4) Details
11052723 Gao JR, Zhu KY: Comparative toxicity of selected organophosphate insecticides against resistant and susceptible clones of the greenbug, Schizaphis graminum (Homoptera: aphididae). J Agric Food Chem. 2000 Oct;48(10):4717-22.

The OR-1 clone showed lower levels of resistance to phenyl (parathion and parathion-methyl) and heterocyclic (chlorpyrifos) OPs than to aliphatic OPs (dimethoate, omethoate, disulfoton, and demeton-S-methyl), whereas the OR-2 clone showed a rather broad spectrum of resistance to nearly all OP insecticides examined.
In vitro inhibition of acetylcholinesterase (AChE) using six selected OP oxon analogues showed that alterations of AChE were involved in resistance to all OP compounds examined in both the OR-1 and OR-2 clones.
3(0,0,0,3) Details
10998265 Charpentier A, Menozzi P, Marcel V, Villatte F, Fournier D: A method to estimate acetylcholinesterase-active sites and turnover in insects. Anal Biochem. 2000 Oct 1;285(1):76-81.

Among the irreversible inhibitors tested, 7-(methylethoxyphosphinyloxy)-1-methylquinolinium iodide, chlorpyrifos-ethyl-oxon, and coumaphos-oxon were found to be sufficiently potent and specific.
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17017223 Cui F, Raymond M, Berthomieu A, Alout H, Weill M, Qiao CL: Recent emergence of insensitive acetylcholinesterase in Chinese populations of the mosquito Culex pipiens (Diptera: Culicidae). J Med Entomol. 2006 Sep;43(5):878-83.

Bioassays performed with a purified G119S strain indicated that this substitution was associated with high levels of resistance to chlorpyrifos, fenitrothion, malathion, and parathion, but low levels of resistance to dichlorvos, trichlorfon, and fenthion.
2(0,0,0,2) Details
12521673 Gordon CJ, Mack CM: Influence of gender on thermoregulation and cholinesterase inhibition in the long-evans rat exposed to diazinon. J Toxicol Environ Health A. 2003 Feb 14;66(3):291-304.

When compared on a molar basis, the hypothermic response to diazinon was relatively small compared to other OPs such as chlorpyrifos.
Diazinon is an organophosphate (OP)-based, anticholinesterase insecticide that irreversibly inhibits acetylcholinesterase activity and produces cholinergic stimulation in central nervous system (CNS) and peripheral tissues.
1(0,0,0,1) Details
15885262 Timchalk C, Poet TS, Hinman MN, Busby AL, Kousba AA: Pharmacokinetic and pharmacodynamic interaction for a binary mixture of chlorpyrifos and diazinon in the rat. Toxicol Appl Pharmacol. 2005 May 15;205(1):31-42.

The primary neurotoxic effects from OP pesticide exposures result from the inhibition of acetylcholinesterase (AChE).
1(0,0,0,1) Details
9439121 Chandre F, Darriet F, Doannio JM, Riviere F, Pasteur N, Guillet P: Distribution of organophosphate and carbamate resistance in Culex pipiens quinquefasciatus (Diptera: Culicidae) in West Africa. J Med Entomol. 1997 Nov;34(6):664-71.

Chlorpyrifos resistance ratios at LC95 ranged from 4 to 30 times in Cote d'Ivoire and from 3 to 6 times in Burkina Faso.
Cross resistance to organophosphates and carbamates was caused by an insensitive acetylcholinesterase allele (AceR).
1(0,0,0,1) Details
18977431 Eells JB, Brown T: Repeated developmental exposure to chlorpyrifos and methyl parathion causes persistent alterations in nicotinic acetylcholine subunit mRNA expression with chlorpyrifos altering dopamine metabolite levels. Neurotoxicol Teratol. 2009 Mar-Apr;31(2):98-103. Epub 2008 Oct 21.

Organophosphates (OPs), commonly used as insecticides, inhibit acetylcholinesterase, the enzyme responsible for the inactivation of synaptic acetylcholine, which results in elevated acetylcholine neurotransmission.
1(0,0,0,1) Details
15550276 Bonfanti P, Colombo A, Orsi F, Nizzetto I, Andrioletti M, Bacchetta R, Mantecca P, Fascio U, Vailati G, Vismara C: Comparative teratogenicity of chlorpyrifos and malathion on Xenopus laevis development. Aquat Toxicol. 2004 Dec 10;70(3):189-200.

We speculate that this muscular damage was related to inhibition of acetylcholinesterase that showed a clear concentration-response in CPF and MTN exposed larvae.
1(0,0,0,1) Details
16449251 Quistad GB, Liang SN, Fisher KJ, Nomura DK, Casida JE: Each lipase has a unique sensitivity profile for organophosphorus inhibitors. Toxicol Sci. 2006 May;91(1):166-72. Epub 2006 Jan 31.

In an overview, inhibition of 28 serine hydrolases (including lipases) by eight OPs (chlorpyrifos oxon, diazoxon, paraoxon, dichlorvos, and four nonpesticides) showed that brain acetylcholinesterase is usually less sensitive than butyrylcholinesterase, liver esterase, cholesterol esterase, and KIAA1363.
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11246135 Mattsson JL, Holden L, Eisenbrandt DL, Gibson JE: Reanalysis with optimized power of red blood cell acetylcholinesterase activity from a 1-year dietary treatment of dogs to chlorpyrifos. Toxicology. 2001 Mar 7;160(1-3):155-64.
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16398125 Romani R, Isani G, De Santis A, Giovannini E, Rosi G: Effects of chlorpyrifos on the catalytic efficiency and expression level of acetylcholinesterases in the bivalve mollusk Scapharca inaequivalvis. Environ Toxicol Chem. 2005 Nov;24(11):2879-86.
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19353435 Mitra NK, Nadarajah VD, Siong HH: Effect of concurrent application of heat, swim stress and repeated dermal application of chlorpyrifos on the hippocampal neurons in mice. Folia Neuropathol. 2009;47(1):60-8.

This study correlates the changes in acetylcholinesterase (AChE) levels and neuronal counts in areas of the hippocampus to consecutive exposure of stress, heat and CPF.
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16978018 Nomura DK, Durkin KA, Chiang KP, Quistad GB, Cravatt BF, Casida JE: Serine hydrolase KIAA1363: toxicological and structural features with emphasis on organophosphate interactions. Chem Res Toxicol. 2006 Sep;19(9):1142-50.

Serine hydrolase KIAA1363 is highly expressed in invasive cancer cells and is the major protein in mouse brain diethylphosphorylated by and hydrolyzing low levels of chlorpyrifos oxon (CPO) (the activated metabolite of a major insecticide).
Studies with knockout mice further show that KIAA1363 partially protects brain AChE and monoacylglycerol lipase from CPO-induced in vivo inhibition.
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15342957 Smulders CJ, Bueters TJ, Vailati S, van Kleef RG, Vijverberg HP: Block of neuronal nicotinic acetylcholine receptors by organophosphate insecticides. Toxicol Sci. 2004 Dec;82(2):545-54. Epub 2004 Sep 1.

Chronic and acute exposure to organophosphate (OP) pesticides may lead to persistent neurological and neurobehavioral effects, which cannot be explained by acetylcholinesterase (AChE) inhibition alone.
Several OP pesticides, e.g., parathion-ethyl, chlorpyrifos and disulfoton, inhibited the ACh-induced ion current with potencies in the micromolar range.
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16243304 Casida JE, Quistad GB: Serine hydrolase targets of organophosphorus toxicants. Chem Biol Interact. 2005 Dec 15;157-158:277-83. Epub 2005 Oct 21.

Acetylcholinesterase (AChE) is one of several hundred serine hydrolases in people potentially exposed to about 80 organophosphorus (OP) compounds important as insecticides or chemical warfare agents.
Pesticides most commonly shown to inhibit these targets in experimental vertebrates are chlorpyrifos and tribufos.
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12642153 Farag AT, El Okazy AM, El-Aswed AF: Developmental toxicity study of chlorpyrifos in rats. Reprod Toxicol. 2003 Mar-Apr;17(2):203-8.

Maternal effects in these groups also included depressed body weight and acetylcholinesterase activity.
1(0,0,0,1) Details
11690566 Barber DS, Ehrich M: Esterase inhibition in SH-SY5Y human neuroblastoma cells following exposure to organophosphorus compounds for 28 days. In Vitr Mol Toxicol. 2001 Summer;14(2):129-35.

To examine metabolic activation in these exposures, pairs of pro- and active toxicants were studied, including chlorpyrifos and its oxon, parathion and paraoxon, and tri-ortho-tolyl phosphate and phenyl saligenin phospahte.
Inhibition of acetylcholinesterase was greater in cells treated for 28 days with all active organophosphorus compounds than it was in cells treated only once with the same concentration of a given OP compound.
1(0,0,0,1) Details
8723267 Wirth MC, Georghiou GP: Organophosphate resistance in Culex pipiens from Cyprus. J Am Mosq Control Assoc. 1996 Mar;12(1):112-8.

All population samples generally revealed organophosphate resistance to malathion, temephos, chlorpyrifos, fenthion, dichlorvos, and pirimiphos methyl, in decreasing order of magnitude.
Resistance was associated with the presence of 5 different overproduced esterases (esterases A1, A2, A5, B2, and B5) as well as an insensitive form of acetylcholinesterase.
1(0,0,0,1) Details
17141929 Marable BR, Maurissen JP, Mattsson JL, Billington R: Differential sensitivity of blood, peripheral, and central cholinesterases in beagle dogs following dietary exposure to chlorpyrifos. Regul Toxicol Pharmacol. 2007 Apr;47(3):240-8. Epub 2006 Dec 4.

Two studies were performed to find out whether exposure limits that protect brain acetylcholinesterase (AChE) will protect peripheral tissue AChE after exposure to chlorpyrifos (CPF), an organophosphate insecticide.
13(0,0,1,8) Details
15045467 Abdel-Rahman A, Dechkovskaia AM, Mehta-Simmons H, Sutton JM, Guan X, Khan WA, Abou-Donia MB: Maternal exposure to nicotine and chlorpyrifos, alone and in combination, leads to persistently elevated expression of glial fibrillary acidic protein in the cerebellum of the offspring in late puberty. Arch Toxicol. 2004 Aug;78(8):467-76. Epub 2004 Mar 26.

Male offspring from mothers treated with either chlorpyrifos or nicotine alone showed a significant increase in the acetylcholinesterase (AChE) activity in the brainstem while female offspring from mothers treated with either nicotine or a combination of nicotine and chlorpyrifos showed a significant increase (approximately 134 and 126% of control, respectively) in AChE activity in the brainstem.
12(0,0,2,2) Details
8913110 Bourguet D, Capela R, Raymond M: An insensitive acetylcholinesterase in Culex pipiens (Diptera:Culicidae) from Portugal. J Econ Entomol. 1996 Oct;89(5):1060-6.

Resistance mechanisms of a strain (PRAIAS) of northern house mosquito, Culex pipiens L., collected in Portugal in 1993, and highly resistant to organophosphates and carbamates, were investigated by comparing the resistance characteristics to 3 organophosphorous (temephos, chlorpyrifos, malathion) and 1 carbamate (propoxur) insecticides in the presence or absence of synergists; and by determining the possible occurrence of overproduced esterases or insensitive acetylcholinesterase (AChE).
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17897769 Buratti FM, Testai E: Evidences for CYP3A4 autoactivation in the desulfuration of dimethoate by the human liver. Toxicology. 2007 Nov 20;241(1-2):33-46. Epub 2007 Aug 6.

It is characterized by low-to-moderate acute mammalian toxicity; similarly to the other OPT pesticides, its mode of action is mediated by the inhibition of acetylcholinesterase (AChE), exerted by its toxic metabolite dimethoate-oxon or omethoate (OME), which is also used as a direct acting pesticide.
This atypical kinetic behaviour can be considered one of the possible explanations for the recent findings that among patients hospitalized following OPT intoxication, DIM ingestion gave different symptoms and more severe poisoning (23.1% of fatal cases versus total) than chlorpyrifos (8% of deaths), which has a lower LD (50) value.
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11534949 Callaghan A, Hirthe G, Fisher T, Crane M: Effect of short-term exposure to chlorpyrifos on developmental parameters and biochemical biomarkers in Chironomus riparius Meigen. Ecotoxicol Environ Saf. 2001 Sep;50(1):19-24.

Acetylcholinesterase activity, glutathione-S-transferase activity, burrowing behavior, emergence time, and adult dry weight were measured to determine which were the most sensitive biomarkers of exposure and effect for short-term sublethal exposures.
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15525694 Peeples ES, Schopfer LM, Duysen EG, Spaulding R, Voelker T, Thompson CM, Lockridge O: Albumin, a new biomarker of organophosphorus toxicant exposure, identified by mass spectrometry. Toxicol Sci. 2005 Feb;83(2):303-12. Epub 2004 Nov 3.

The classical laboratory tests for exposure to organophosphorus toxicants (OP) are inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activity in blood.
In vitro experiments with human plasma showed that chlorpyrifos oxon, echothiophate, malaoxon, paraoxon, methyl paraoxon, diazoxon, diisopropylfluorophosphate, and dichlorvos competed with FP-biotin for binding to human albumin.
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17190973 Carvajal F, Lopez-Grancha M, Navarro M, Sanchez-Amate Mdel C, Cubero I: Long-lasting reductions of ethanol drinking, enhanced ethanol-induced sedation, and decreased c-fos expression in the Edinger-Westphal nucleus in Wistar rats exposed to the organophosphate chlorpyrifos. Toxicol Sci. 2007 Apr;96(2):310-20. Epub 2006 Dec 26.

We hypothesize that CPF might modulate cellular mechanisms (decreased intracellular cAMP signaling, alpha-7-nicotinic receptors, and/or cerebral acetylcholinesterase inhibition) in neuronal pathways critically involved in neurobiological responses to ethanol.
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11749124 Karanth S, Olivier K Jr, Liu J, Pope C: In vivo interaction between chlorpyrifos and parathion in adult rats: sequence of administration can markedly influence toxic outcome. Toxicol Appl Pharmacol. 2001 Dec 15;177(3):247-55.

Organophosphorus insecticides (OPs) generally act through a common mechanism of toxicity initiated by inhibition of acetylcholinesterase (AChE).
1(0,0,0,1) Details
18026775 Jin-Clark Y, Anderson TD, Zhu KY: Effect of alachlor and metolachlor on toxicity of chlorpyrifos and major detoxification enzymes in the aquatic midge, Chironomus tentans (Diptera: Chironomidae). Arch Environ Contam Toxicol. 2008 May;54(4):645-52. Epub 2007 Nov 17.

Furthermore, alachlor and metolachlor at 1,000 microg/L reduced acetylcholinesterase (AChE) activity by 34.3% and 27.6%, respectively, in the treated midges.
1(0,0,0,1) Details
17067049 Zayed AB, Szumlas DE, Hanafi HA, Fryauff DJ, Mostafa AA, Allam KM, Brogdon WG: Use of bioassay and microplate assay to detect and measure insecticide resistance in field populations of Culex pipiens from filariasis endemic areas of Egypt. J Am Mosq Control Assoc. 2006 Sep;22(3):473-82.

Microplate assays were performed to measure levels of beta esterase, acetylcholinesterase, insensitive acetylcholinesterase, oxidases, and glutathione-S-transferase enzymes.
The Qalubiya larval population was susceptible only to malathion, whereas Sharkiya larvae were susceptible to malathion, temephos, and chlorpyrifos.
1(0,0,0,1) Details
15918909 Asidi AN, N'Guessan R, Koffi AA, Curtis CF, Hougard JM, Chandre F, Corbel V, Darriet F, Zaim M, Rowland MW: Experimental hut evaluation of bednets treated with an organophosphate (chlorpyrifos-methyl) or a pyrethroid (lambdacyhalothrin) alone and in combination against insecticide-resistant Anopheles gambiae and Culex quinquefasciatus mosquitoes. Malar J. 2005 May 26;4(1):25.

Anopheles gambiae and Culex quinquefasciatus mosquitoes from the area are resistant to pyrethroids and organophosphates (kdr and insensitive acetylcholinesterase Ace.1R).
1(0,0,0,1) Details
15180375 Printes LB, Callaghan A: A comparative study on the relationship between acetylcholinesterase activity and acute toxicity in Daphnia magna exposed to anticholinesterase insecticides. Environ Toxicol Chem. 2004 May;23(5):1241-7.

Acetylcholinesterase (AChE) activity was measured in Daphnia magna that had been exposed to four organophosphates (OPs; parathion, chlorpyrifos, malathion, and acephate) and one carbamate (propoxur) for 48 h.
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20000004 Ghedira J, Jebali J, Bouraoui Z, Banni M, Chouba L, Boussetta H: Acute effects of chlorpyryphos-ethyl and secondary treated effluents on acetylcholinesterase and butyrylcholinesterase activities in Carcinus maenas. J Environ Sci. 2009;21(10):1467-72.

The acute effects of commercial formulation of chlorpyrifos-ethyl (Dursban) and the secondary treated industrial/urban effluent (STIUE) exposure on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) activities in hepatopancreas and gills of Mediterranean crab Carcinus maenas were investigated.
10(0,0,1,5) Details
16289700 Abdel-Halim KY, Salama AK, El-Khateeb EN, Bakry NM: Organophosphorus pollutants (OPP) in aquatic environment at Damietta Governorate, Egypt: implications for monitoring and biomarker responses. Chemosphere. 2006 Jun;63(9):1491-8. Epub 2005 Nov 14.

The obtained results are in parallel to that found in case of cholinesterase activity where the activity of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) was declined at these seasonal period.
Chlorpyrifos, chlorpyrifos-methyl, malathion, diazinon, pirimiphos-methyl and profenofos were detected in most samples.
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18968616 Andreescu S, Noguer T, Magearu V, Marty JL: Screen-printed electrode based on AChE for the detection of pesticides in presence of organic solvents. Talanta. 2002 Apr 22;57(1):169-76.

Detection limits as low as 1.91x10 (-8) M paraoxon and 1.24x10 (-9) M chlorpyrifos ethyl oxon were obtained when experiments are carried out in 5% acetonitrile.
3(0,0,0,3) Details
7539166 Li WF, Furlong CE, Costa LG: Paraoxonase protects against chlorpyrifos toxicity in mice. Toxicol Lett. 1995 Apr;76(3):219-26.

Inhibition of acetylcholinesterase (AChE) in brain, diaphragm, plasma and red blood cells was measured as an index of CPS (100 mg/kg) toxicity.
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12140181 Schuh RA, Lein PJ, Beckles RA, Jett DA: Noncholinesterase mechanisms of chlorpyrifos neurotoxicity: altered phosphorylation of Ca2+/cAMP response element binding protein in cultured neurons. Toxicol Appl Pharmacol. 2002 Jul 15;182(2):176-85.

We further tested the hypothesis that changes in CREB occur independent of AChE inhibition.
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13678652 Ricceri L, Markina N, Valanzano A, Fortuna S, Cometa MF, Meneguz A, Calamandrei G: Developmental exposure to chlorpyrifos alters reactivity to environmental and social cues in adolescent mice. Toxicol Appl Pharmacol. 2003 Sep 15;191(3):189-201.

Brain acetylcholinesterase (AChE) activity was evaluated within 24 h from termination of treatments.
2(0,0,0,2) Details
11350214 Quistad GB, Sparks SE, Casida JE: Fatty acid amide hydrolase inhibition by neurotoxic organophosphorus pesticides. Toxicol Appl Pharmacol. 2001 May 15;173(1):48-55.

Chlorpyrifos oxon inhibits 50% of the FAAH activity (IC50 at 15 min, 25 degrees C, pH 9.0) in vitro at 40--56 nM for mouse brain and liver, whereas methyl arachidonyl phosphonofluoridate, ethyl octylphosphonofluoridate (EOPF), oleyl-4H-1,3,2-benzodioxaphosphorin 2-oxide (oleyl-BDPO), and dodecyl-BDPO give IC50s of 0.08--1.1 nM.
These BDPOs and EOPF inhibit mouse brain FAAH in vitro with > or =200-fold higher potency than for AChE.
1(0,0,0,1) Details
11750078 Howard MD, Pope CN: In vitro effects of chlorpyrifos, parathion, methyl parathion and their oxons on cardiac muscarinic receptor binding in neonatal and adult rats. Toxicology. 2002 Jan 15;170(1-2):1-10.

Organophosphorus insecticides elicit toxicity by inhibiting acetylcholinesterase.
1(0,0,0,1) Details
19079407 Paudyal BP: Organophosphorus poisoning. JNMA J Nepal Med Assoc. 2008 Oct-Dec;47(172):251-8.

Metacid (Methyl parathion) and Nuvan (Dichlorovos) are commonly ingested OP pesticides; Dimethoate, Profenofos, and Chlorpyrifos are other less frequently ingested compounds in Nepal.
The toxicity of these OP pesticides is due to the irreversible inhibition of acetylcholinesterase (AChE) enzyme leading to accumulation of acetylcholine and subsequent over-activation of cholinergic receptors in various parts of the body.
1(0,0,0,1) Details
19680979 Jensen BH, Petersen A, Christensen T: Probabilistic assessment of the cumulative dietary acute exposure of the population of Denmark to organophosphorus and carbamate pesticides. Food Addit Contam Part A Chem Anal Control Expo Risk Assess. 2009 Jul;26(7):1038-48.

We calculated the cumulative acute exposure to 1.8% and 0.8% of the acute reference dose (ARfD) of 100 microg kg (-1) body weight (bw) day (-1) of chlorpyrifos as an index compound at the 99.9th percentile (P99.5) for children and adults, respectively.
Organophosphorus and carbamate pesticides are acetylcholinesterase-inhibiting pesticides and as such have a common mode of action.
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11350209 Cowan J, Sinton CM, Varley AW, Wians FH, Haley RW, Munford RS: Gene therapy to prevent organophosphate intoxication. Toxicol Appl Pharmacol. 2001 May 15;173(1):1-6.

To test whether boosting serum levels of PON1 enzymes by gene therapy might provide increased protection, we compared the degree of inactivation of whole brain acetylcholinesterase of mice exposed to chlorpyrifos 4 days after intravenous injection of recombinant adenoviruses containing PON1-LQ or PON1-LR genes or no PON1 gene.
Both recombinant viruses containing PON1 genes boosted serum arylesterase concentrations by approximately 60% and significantly prevented the inactivation of brain acetylcholinesterase.
1(0,0,0,1) Details
7689993 Richardson RJ, Moore TB, Kayyali US, Randall JC: Chlorpyrifos: assessment of potential for delayed neurotoxicity by repeated dosing in adult hens with monitoring of brain acetylcholinesterase, brain and lymphocyte neurotoxic esterase, and plasma butyrylcholinesterase activities. Fundam Appl Toxicol. 1993 Jul;21(1):89-96.
9(0,0,1,4) Details
15018574 Schulze H, Schmid RD, Bachmann TT: Activation of phosphorothionate pesticides based on a cytochrome P450 BM-3 (CYP102 A1) mutant for expanded neurotoxin detection in food using acetylcholinesterase biosensors. Anal Chem. 2004 Mar 15;76(6):1720-5.

The application of the method to infant food in combination with a disposable AChE biosensor enabled detection of chlorpyrifos and parathion at concentrations down to 20 microg/kg within an overall assay time of 95 min.
9(0,0,1,4) Details
17521148 Tierney K, Casselman M, Takeda S, Farrell T, Kennedy C: The relationship between cholinesterase inhibition and two types of swimming performance in chlorpyrifos-exposed coho salmon (Oncorhynchus kisutch). Environ Toxicol Chem. 2007 May;26(5):998-1004.

Brain acetylcholinesterase (AChE) activity was evaluated after two different swimming tests in coho salmon (Oncorhynchus kisutch; 238 +/- 5 g) given 96-h exposures to 0, 5, 10, 20, or 40 microg/L of chlorpyrifos.
9(0,0,1,4) Details
19680907 Chen C, Li Y, Chen M, Chen Z, Qian Y: Organophosphorus pesticide residues in milled rice (Oryza sativa) on the Chinese market and dietary risk assessment. Food Addit Contam Part A Chem Anal Control Expo Risk Assess. 2009 Mar;26(3):340-7.

The present study investigates the occurrence of acetylcholinesterase (AChE)-inhibiting organophosphorus (OP) pesticide residues in milled rice samples obtained form local markets in China during the period 2004-2006 and estimates their cumulative exposure.
The results showed that 9.3% of the samples contained detectable residues of at least one of the seven target OP pesticides (chlorpyrifos, dichlorvos, omethoate, methamidophos, parathion-methyl, parathion and triazophos) mainly used for agriculture in China, with concentrations ranging 0.011-1.756 mg kg (-1).
3(0,0,0,3) Details
17644233 Howard MD, Mirajkar N, Karanth S, Pope CN: Comparative effects of oral chlorpyrifos exposure on cholinesterase activity and muscarinic receptor binding in neonatal and adult rat heart. Toxicology. 2007 Sep 5;238(2-3):157-65. Epub 2007 Jun 14.

Organophosphorus (OP) pesticides elicit acute toxicity by inhibiting acetylcholinesterase (AChE), the enzyme responsible for inactivating acetylcholine (ACh) at cholinergic synapses.
3(0,0,0,3) Details
12109753 Anderson TD, Lydy MJ: Increased toxicity to invertebrates associated with a mixture of atrazine and organophosphate insecticides. Environ Toxicol Chem. 2002 Jul;21(7):1507-14.

This study examined the joint toxicity of atrazine and three organophosphate (OP) insecticides (chlorpyrifos, methyl parathion, and diazinon) exposed to Hyalella azteca and Musca domestica.
Acetylcholinesterase (AChE) activity also was examined for the individual OPs with and without atrazine treatment.
2(0,0,0,2) Details
18187192 Roh JY, Choi J: Ecotoxicological evaluation of chlorpyrifos exposure on the nematode Caenorhabditis elegans. Ecotoxicol Environ Saf. 2008 Oct;71(2):483-9. Epub 2008 Jan 9.

To assess the molecular-level effect, stress-related gene expression was investigated, and the neurotoxicity indicator, acetylcholinesterase (AChE) activity was assessed as the biochemical-level response.
2(0,0,0,2) Details
17824663 Walz I, Schwack W: Cutinase inhibition by means of insecticidal organophosphates and carbamates. 3. J Agric Food Chem. 2007 Oct 3;55(20):8177-86. Epub 2007 Sep 8.

Chloroperoxidase (CPO) from Caldariomyces fumago combined with hydrogen peroxide and chloride proved to be most efficient for the transformation of organophosphorothionate pesticides, i.e., chlorpyrifos, chlorpyrifos-methyl, parathion, and parathion-methyl, into their more potent serine esterase inhibiting oxon analogues.
This type of enzymatic oxidation is easier to perform and more efficient, as compared to bromine or N-bromosuccinimide, used for acetylcholine esterase (AChE) assay in water analyses, but is insufficient for complex matrices such as plant sample extracts.
1(0,0,0,1) Details
11712994 Boone JS, Tyler JW, Chambers JE: Transferable residues from dog fur and plasma cholinesterase inhibition in dogs treated with a flea control dip containing chlorpyrifos. Environ Health Perspect. 2001 Nov;109(11):1109-14.

The pretreatment specific activities in the plasma of the dogs were about 75 nmol/min/mg protein for butyrylcholinesterase (BChE), and 9 nmol/min/mg protein for acetylcholinesterase (AChE).
1(0,0,0,1) Details
20329403 Akhtar N, Srivastava MK, Raizada RB: Assessment of chlorpyrifos toxicity on certain organs in rat, Rattus norvegicus. J Environ Biol. 2009 Nov;30(6):1047-53.

A dose dependent inhibition of acetylcholinesterase (AChE) activity in RBC (22-60%) and brain (7-52%) was observed.
1(0,0,0,1) Details
9299188 Chanda SM, Mortensen SR, Moser VC, Padilla S: Tissue-specific effects of chlorpyrifos on carboxylesterase and cholinesterase activity in adult rats: an in vitro and in vivo comparison. Fundam Appl Toxicol. 1997 Aug;38(2):148-57.

Organophosphate (OP) pesticides can bind to carboxylesterase (CaE), which may lower the concentration of OPs at the target site enzyme, acetylcholinesterase (ChE).
1(0,0,0,1) Details
16004201 Fujikawa Y, Satoh T, Suganuma A, Suzuki S, Niikura Y, Yui S, Yamaura Y: Extremely sensitive biomarker of acute organophosphorus insecticide exposure. Hum Exp Toxicol. 2005 Jun;24(6):333-6.

Thus, the single administration of EPN (O-ethyl O-p-nitrophenylphenylphosphonothioate), acephate and chlorpyrifos increased plasma BG activity in approximately 100-fold the control level in rats.
The increase in plasma BG activity after OP exposure is a much more sensitive biomarker of acute OP exposure than acetylcholinesterase (AChE) inhibition.
1(0,0,0,1) Details
7566687 Huff RA, Abou-Donia MB: In vitro effect of chlorpyrifos oxon on muscarinic receptors and adenylate cyclase. Neurotoxicology. 1995 Summer;16(2):281-90.

Although the neurotoxicity of organophosphorus compounds is generally attributed to inhibition of acetylcholinesterase, recent reports have indicated that direct interactions with muscarinic receptors and signal transduction may be an additional mechanism of neurotoxicity.
1(0,0,0,1) Details
15112752 Knaak JB, Dary CC, Power F, Thompson CB, Blancato JN: Physicochemical and biological data for the development of predictive organophosphorus pesticide QSARs and PBPK/PD models for human risk assessment. Crit Rev Toxicol. 2004 Mar-Apr;34(2):143-207.

Except for work on parathion, chlorpyrifos, and isofenphos, very few modeling data were found on the 31 OPs of interest.
A limited amount of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and carboxylesterase (CaE) inhibition and recovery data were found in the literature on the 31 OPs.
1(0,0,0,1) Details
19662716 Ramesh H, David M: Respiratory performance and behavioral responses of the freshwater fish, Cyprinus carpio (Linnaeus) under sublethal chlorpyrifos exposure. J Basic Clin Physiol Pharmacol. 2009;20(2):127-39.

The behavioral and morphologic changes might be due to the inhibition of acetylcholinesterase (AChE) activity.
1(0,0,0,1) Details
9292287 Worek F, Backer M, Thiermann H, Szinicz L, Mast U, Klimmek R, Eyer P: Reappraisal of indications and limitations of oxime therapy in organophosphate poisoning. Hum Exp Toxicol. 1997 Aug;16(8):466-72.

These data may help to define more precisely the indications and limitations of oxime therapy in organophosphate (OP) poisoning. 2 Diethylphosphoryl-AChE resulting from intoxications with parathion, chlorpyrifos, chlorfenvinphos, diazinon and other OPs is characterized by slow spontaneous reactivation and low propensity for ageing.
9(0,0,1,4) Details
14759667 El-Merhibi A, Kumar A, Smeaton T: Role of piperonyl butoxide in the toxicity of chlorpyrifos to Ceriodaphnia dubia and Xenopus laevis. Ecotoxicol Environ Saf. 2004 Feb;57(2):202-12.

Acetylcholinesterase (AChE) activity was used as a biomarker to further assess the role of PBO in chlorpyrifos toxicity.
8(0,0,1,3) Details
11332849 Byrne FJ, Toscano NC: An insensitive acetylcholinesterase confers resistance to methomyl in the beet armyworm Spodoptera exigua (Lepidoptera: Noctuidae). J Econ Entomol. 2001 Apr;94(2):524-8.

In biochemical studies, the BKRR AChE enzyme was approximately 30-fold and sixfold more insensitive to methomyl and chlorpyrifos-oxon, respectively, compared with the DOW enzyme.
8(0,0,1,3) Details
16515465 Kuca K, Juna D, Musilek K: Structural requirements of acetylcholinesterase reactivators. Mini Rev Med Chem. 2006 Mar;6(3):269-77.

Nerve agents (sarin, soman, cyclosarin, tabun and VX agent) and pesticides (paraoxon, chlorpyrifos, TEPP) represent extremely toxic group of organophosphorus compounds (OPCs).
8(0,0,0,8) Details
16640555 Amitai G, Gaidukov L, Adani R, Yishay S, Yacov G, Kushnir M, Teitlboim S, Lindenbaum M, Bel P, Khersonsky O, Tawfik DS, Meshulam H: Enhanced stereoselective hydrolysis of toxic organophosphates by directly evolved variants of mammalian serum paraoxonase. FEBS J. 2006 May;273(9):1906-19.

Subsequently, nine directly evolved PON1 variants, selected for increased hydrolytic rates with a fluorogenic diethylphosphate ester, were tested for detoxification of cyclosarin, soman, O-isopropyl-O-(p-nitrophenyl) methyl phosphonate (IMP-pNP), DFP, and chlorpyrifos-oxon (ChPo).
Detoxification rates were determined by temporal acetylcholinesterase inhibition by residual nonhydrolyzed OP.
3(0,0,0,3) Details
19269805 Viswanathan S, Radecka H, Radecki J: Electrochemical biosensor for pesticides based on acetylcholinesterase immobilized on polyaniline deposited on vertically assembled carbon nanotubes wrapped with ssDNA. Biosens Bioelectron. 2009 May 15;24(9):2772-7. Epub 2009 Feb 10.

An electrochemical biosensor for the determination of pesticides: methyl parathion and chlorpyrifos, two of the most commonly used organophosphorous insecticides in vegetable crops, is described.
3(0,0,0,3) Details
18164358 Nomura DK, Fujioka K, Issa RS, Ward AM, Cravatt BF, Casida JE: Dual roles of brain serine hydrolase KIAA1363 in ether lipid metabolism and organophosphate detoxification. Toxicol Appl Pharmacol. 2008 Apr 1;228(1):42-8. Epub 2007 Dec 3.

KIAA1363 was the primary AcMAGE hydrolase in brain, lung, heart and kidney and was highly sensitive to inactivation by chlorpyrifos oxon (CPO) (IC50 2 nM) [the bioactivated metabolite of the major insecticide chlorpyrifos (CPF)].
On considering detoxification, KIAA1363 -/- mice were significantly more sensitive than +/+ mice to ip-administered CPF (100 mg/kg) and parathion (10 mg/kg) with increased tremoring and mortality that correlated for CPF with greater brain acetylcholinesterase inhibition.
1(0,0,0,1) Details
19632257 Grigoryan H, Schopfer LM, Peeples ES, Duysen EG, Grigoryan M, Thompson CM, Lockridge O: Mass spectrometry identifies multiple organophosphorylated sites on tubulin. Toxicol Appl Pharmacol. 2009 Oct 15;240(2):149-58. Epub 2009 Jul 24.

Acute toxicity of organophosphorus poisons (OP) is explained by inhibition of acetylcholinesterase in nerve synapses.
Pure bovine tubulin (0.012 mM) was treated with 0.01-0.5 mM chlorpyrifos oxon for 24 h at 37 degrees C in pH 8.3 buffer.
1(0,0,0,1) Details
19165396 Tait S, Ricceri L, Venerosi A, Maranghi F, Mantovani A, Calamandrei G: Long-term effects on hypothalamic neuropeptides after developmental exposure to chlorpyrifos in mice. Environ Health Perspect. 2009 Jan;117(1):112-6. Epub 2008 Aug 22.

Dose levels were chosen to avoid systemic toxicity and inhibition of brain acetylcholinesterase.
1(0,0,0,1) Details
12452633 Del Carlo M, Mascini M, Pepe A, Compagnone D, Mascini M: Electrochemical bioassay for the investigation of chlorpyrifos-methyl in vine samples. J Agric Food Chem. 2002 Dec 4;50(25):7206-10.

The analytical method was based on electrochemical determination of the extent of the inhibition exerted by the pesticide on acetylcholinesterase using the substrate acetylthiocholine.
1(0,0,0,1) Details
9620094 Geller AM, Abdel-Rahman AA, Peiffer RL, Abou-Donia MB, Boyes WK: The organophosphate pesticide chlorpyrifos affects form deprivation myopia. Invest Ophthalmol Vis Sci. 1998 Jun;39(7):1290-4.

RESULTS: Dosing with CPF yielded an inhibition of 35% butyrylcholinesterase in plasma and 45% acetylcholinesterase in brain.
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17615116 Carter WG, Tarhoni M, Rathbone AJ, Ray DE: Differential protein adduction by seven organophosphorus pesticides in both brain and thymus. Hum Exp Toxicol. 2007 Apr;26(4):347-53.


We found significant adduction of partially characterized protein targets in both rat brain and thymus by azamethiphos, chlorfenvinphos, chlorpyrifos-oxon, diazinon-oxon, dichlorvos and malaoxon, in vitro and pirimiphos-methyl in vivo.
0(0,0,0,0) Details
18417317 Sachana M, Flaskos J, Sidiropoulou E, Yavari CA, Hargreaves AJ: Inhibition of extension outgrowth in differentiating rat C6 glioma cells by chlorpyrifos and chlorpyrifos oxon: effects on microtubule proteins. Toxicol In Vitro. 2008 Aug;22(5):1387-91. Epub 2008 Mar 18.

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11083088 Bomser J, Casida JE: Activation of extracellular signal-regulated kinases (ERK 44/42) by chlorpyrifos oxon in Chinese hamster ovary cells. J Biochem Mol Toxicol. 2000;14(6):346-53.

0(0,0,0,0) Details
1719272 Pence BC, Demick DS, Richard BC, Buddingh F: The efficacy and safety of chlorpyrifos (Dursban) for control of Myobia musculi infestation in mice. Lab Anim Sci. 1991 Apr;41(2):139-42.

0(0,0,0,0) Details
15764539 Bouchard M, Carrier G, Brunet RC, Bonvalot Y, Gosselin NH: Determination of biological reference values for chlorpyrifos metabolites in human urine using a toxicokinetic approach. J Occup Environ Hyg. 2005 Mar;2(3):155-68.

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11875622 Ashry KM, Abu-Qare AW, Saleem FR, Hussein YA, Hamza SM, Kishk AM, Abou-Donia MB: Inhibition and recovery of maternal and fetal cholinesterase enzymes following a single oral dose of chlorpyrifos in rats. Arch Toxicol. 2002 Feb;76(1):30-9. Epub 2001 Dec 18.

Maternal and fetal brain acetylcholinesterase (AchE) and plasma butyrylcholinesterase (BuChE) activities were significantly inhibited 1 h after treatment.
8(0,0,0,8) Details
16085276 Binelli A, Ricciardi F, Riva C, Provini A: New evidences for old biomarkers: effects of several xenobiotics on EROD and AChE activities in Zebra mussel (Dreissena polymorpha). Chemosphere. 2006 Jan;62(4):510-9. Epub 2005 Aug 8.

The aim of this research was to investigate changes on EROD and AChE activities in the freshwater bivalve Zebra mussel (Dreissena polymorpha) exposed to different pollutants (Arochlor 1260, CB 153 and 126, pp'DDT, chlorpyrifos, carbaryl) at laboratory conditions, in order to standardize the analytical procedures and to highlight eventual interferences on enzyme activities.
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16960032 Hoogduijn MJ, Rakonczay Z, Genever PG: The effects of anticholinergic insecticides on human mesenchymal stem cells. Toxicol Sci. 2006 Dec;94(2):342-50. Epub 2006 Sep 7.

Organophosphate (OP) and carbamate pesticides, which are used in large amounts in agriculture to control insects, are designed to disrupt acetylcholine signaling by inhibiting the enzyme acetylcholinesterase (AChE).
We therefore examined the effects of an OP pesticide, chlorpyrifos, and a carbamate, carbofuran, on MSC characteristics.
3(0,0,0,3) Details
14679985 Key PB, Fulton MH, Harman-Fetcho JA, McConnell LL: Acetylcholinesterase activity in grass shrimp and aqueous pesticide levels from South Florida drainage canals. Arch Environ Contam Toxicol. 2003 Oct;45(3):371-7.

Three organophosphate insecticides (chlorpyrifos, malathion, diazinon) were detected at three sites in two canals (Military and North).
3(0,0,0,3) Details
17350100 Lopez-Crespo GA, Carvajal F, Flores P, Sanchez-Santed F, Sanchez-Amate MC: Time course of biochemical and behavioural effects of a single high dose of chlorpyrifos. Neurotoxicology. 2007 May;28(3):541-7. Epub 2007 Feb 4.

For this, the study was divided in two phases; in the first phase, we studied the time course of the effects produced by treatment with a high dose of CPF (250 mg/kg s.c.) on rat locomotor activity and anxiety behaviours recorded on an open-field, as well as on AChE inhibition.
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15081265 Karanth S, Liu J, Olivier K Jr, Pope C: Interactive toxicity of the organophosphorus insecticides chlorpyrifos and methyl parathion in adult rats. Toxicol Appl Pharmacol. 2004 Apr 15;196(2):183-90.

These findings suggest that the sequence of exposure to two insecticides that elicit toxicity through a common mechanism can markedly influence the cumulative action at the target site (acetylcholinesterase, AChE) and consequent functional toxicity.
1(0,0,0,1) Details
10774652 Karunaratne SH: Insecticide cross-resistance spectra and underlying resistance mechanisms of Sri Lankan anopheline vectors of malaria. Southeast Asian J Trop Med Public Health. 1999 Sep;30(3):460-9.

Adult mosquitos were individually tested for their insecticide detoxifying enzyme activities and altered target-site, acetylcholinesterase.
Adult and larval bioassays were carried out to obtain log-probit mortality lines for malathion, propoxur, permethrin and chlorpyrifos.
1(0,0,0,1) Details
15207377 Jacobsen H, Ostergaard G, Lam HR, Poulsen ME, Frandsen H, Ladefoged O, Meyer O: Repeated dose 28-day oral toxicity study in Wistar rats with a mixture of five pesticides often found as residues in food: alphacypermethrin, bromopropylate, carbendazim, chlorpyrifos and mancozeb. Food Chem Toxicol. 2004 Aug;42(8):1269-77.

Plasma acetylcholinesterase was significantly decreased in the groups 2, 5 and 6 males.
1(0,0,0,1) Details
16760416 Ricceri L, Venerosi A, Capone F, Cometa MF, Lorenzini P, Fortuna S, Calamandrei G: Developmental neurotoxicity of organophosphorous pesticides: fetal and neonatal exposure to chlorpyrifos alters sex-specific behaviors at adulthood in mice. Toxicol Sci. 2006 Sep;93(1):105-13. Epub 2006 Jun 7.

Serum and brain acetylcholinesterase (AChE) activity was evaluated at birth and 24 h from termination of postnatal treatments.
1(0,0,0,1) Details
15888665 Quistad GB, Klintenberg R, Casida JE: Blood acylpeptide hydrolase activity is a sensitive marker for exposure to some organophosphate toxicants. Toxicol Sci. 2005 Aug;86(2):291-9. Epub 2005 May 11.

The most potent in vitro inhibitors for human erythrocyte and mouse brain APH are DFP (IC (50) 11-17 nM), chlorpyrifos oxon (IC (50) 21-71 nM), dichlorvos (IC (50) 230-560 nM), naled (IC (50) 370-870 nM), and their analogs with modified alkyl substituents. (3) H-diisopropyl fluorophosphate is a potent inhibitor of mouse blood and brain APH in vivo (ED (50) 0.09-0.2 mg/kg and 0.02-0.03 mg/l for ip and vapor exposure, respectively).
Sarin administered ip at a lethal dose to guinea pigs inhibits blood acetylcholinesterase and BChE completely but erythrocyte APH only partially.
1(0,0,0,1) Details
17110060 Buratti FM, Leoni C, Testai E: Foetal and adult human CYP3A isoforms in the bioactivation of organophosphorothionate insecticides. Toxicol Lett. 2006 Dec 15;167(3):245-55. Epub 2006 Oct 24.


Since OPT-induced neurodevelopmental effects may be due to in situ bioactivation by foetal enzymes, the catalytic activity of the foetal CYP3A7 toward chlorpyrifos (CPF), parathion (PAR), malathion (MAL) and fenthion (FEN) has been assessed by using recombinant enzymes.
0(0,0,0,0) Details
15546633 Booth GM, Mortensen SR, Carter MW, Schaalje BG: Hazard evaluation for northern bobwhite quail (Colinus virginianus) exposed to chlorpyrifos-treated turf and seed. Ecotoxicol Environ Saf. 2005 Feb;60(2):176-87.

0(0,0,0,0) Details
10048149 Barber D, Correll L, Ehrich M: Comparison of two in vitro activation systems for protoxicant organophosphorous esterase inhibitors. Toxicol Sci. 1999 Jan;47(1):16-22.


Incubation of parathion or chlorpyrifos with 0.05% bromine solution or uninduced rat liver microsomes (RLM) resulted in production of the corresponding oxygen analogs of these OP compounds and markedly increased esterase inhibition in SH-SY5Y human neuroblastoma cells.
0(0,0,0,0) Details
11781077 Bomser JA, Quistad GB, Casida JE: Chlorpyrifos oxon potentiates diacylglycerol-induced extracellular signal-regulated kinase (ERK 44/42) activation, possibly by diacylglycerol lipase inhibition. Toxicol Appl Pharmacol. 2002 Jan 1;178(1):29-36.

0(0,0,0,0) Details
16011852 Wheelock CE, Eder KJ, Werner I, Huang H, Jones PD, Brammell BF, Elskus AA, Hammock BD: Individual variability in esterase activity and CYP1A levels in Chinook salmon (Oncorhynchus tshawytscha) exposed to esfenvalerate and chlorpyrifos. Aquat Toxicol. 2005 Aug 30;74(2):172-92.

In this study, carboxylesterase and AChE activity, cytochrome P4501A (CYP1A) protein levels, and mortality were measured in individual juvenile Chinook salmon (Oncorhynchus tshawytscha) following exposure to an OP (chlorpyrifos) and a pyrethroid (esfenvalerate).
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18716607 Garabrant DH, Aylward LL, Berent S, Chen Q, Timchalk C, Burns CJ, Hays SM, Albers JW: Cholinesterase inhibition in chlorpyrifos workers: Characterization of biomarkers of exposure and response in relation to urinary TCPy. J Expo Sci Environ Epidemiol. 2009 Nov;19(7):634-42. Epub 2008 Aug 20.

The objective of this study was to evaluate the quantitative relation between measured red blood cell acetylcholinesterase (RBC AChE) and plasma butyrylcholinesterase (BuChE) activities with exposure to chlorpyrifos (CPF) as assessed by measurement of urinary 3,5,6-trichloro-2-pyridinol (TCPy) in a study group of workers occupationally exposed in the manufacture of CPF and a referent group of chemical manufacturing workers.
8(0,0,1,3) Details
18072155 Mohammad FK, Alias AS, Ahmed OA: Electrometric measurement of plasma, erythrocyte, and whole blood cholinesterase activities in healthy human volunteers. J Med Toxicol. 2007 Mar;3(1):25-30.

Following in vitro inhibition of pseudo cholinesterase by quinidine sulfate, true cholinesterase activity was estimated in the plasma of the subjects.
After in vitro addition of the organophosphate (chlorpyrifos and methidathion, 0.5 and 1 microM) and carbamate (carbaryl, 5 and 10 microM) insecticides to the reaction mixtures, inhibitions of blood cholinesterases were measured.
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16343621 Key PB, Fulton MH: Correlation between 96-h mortality and 24-h acetylcholinesterase inhibition in three grass shrimp larval life stages. Ecotoxicol Environ Saf. 2006 Mar;63(3):389-92. Epub 2005 Dec 15.

In the chlorpyrifos exposures, newly hatched larvae and postlarvae were the most sensitive life stages.
3(0,0,0,3) Details
1375016 Vasilic Z, Drevenkar V, Rumenjak V, Stengl B, Frobe Z: Urinary excretion of diethylphosphorus metabolites in persons poisoned by quinalphos or chlorpyrifos. Arch Environ Contam Toxicol. 1992 May;22(4):351-7.

The most rapid increase in red blood cell acetylcholinesterase activity was noted within 24 h after the first treatment with oximes Pralidoxime and/or HI-6.
1(0,0,0,1) Details
9685989 Rodriguez MM, Bisset J, Rodriguez I, Diaz C: [Determination of insecticide resistance and its biochemical mechanisms in 2 strains of Culex quinquefasciatus from Santiago de Cuba]. Rev Cubana Med Trop. 1997;49(3):209-14.


It was determined by the biochemical tests that there existed a high frequency of the mechanisms of esterases and altered acetylcholinesterase.
1(0,0,0,1) Details
12453664 Wu YJ, Harp P, Yan XR, Pope CN: Nicotinic autoreceptor function in rat brain during maturation and aging: possible differential sensitivity to organophosphorus anticholinesterases. Chem Biol Interact. 2003 Jan 6;142(3):255-68.

The active metabolite of CPF (i.e. chlorpyrifos oxon (CPO), 1-10 microM) inhibited NAF in vitro.
Together these data suggest that NAF is differentially expressed during maturation and that this neuromodulatory process may be selectively altered by some OP insecticides, potentially contributing to age-related differences in response to AChE inhibitors.
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18394709 Timchalk C, Poet TS: Development of a physiologically based pharmacokinetic and pharmacodynamic model to determine dosimetry and cholinesterase inhibition for a binary mixture of chlorpyrifos and diazinon in the rat. Neurotoxicology. 2008 May;29(3):428-43. Epub 2008 Mar 10.

It is anticipated that these OPs could interact at a number of important metabolic steps including: CYP450 mediated activation/detoxification, B-esterases [carboxylesterase (CaE), butyrylcholinesterase (BuChE) and acetylcholinesterase (AChE)] or PON-1 (A-esterase) oxon detoxification.
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17532548 Xuereb B, Noury P, Felten V, Garric J, Geffard O: Cholinesterase activity in Gammarus pulex (Crustacea Amphipoda): characterization and effects of chlorpyrifos. Toxicology. 2007 Jul 17;236(3):178-89. Epub 2007 Apr 24.

In vivo AChE inhibition was observed at realistic environmental concentrations, with lethal effects appearing at inhibitions higher than 50%.
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11107890 Diaz C, Perez M, Rodriguez MM, Calvo E, Bisset JA, Fresneda M: [Resistance to insecticides in Blattella germanica species strains from Santiago de Cuba]. Rev Cubana Med Trop. 2000 Jan-Apr;52(1):24-30.


A study was conducted on the level of resistance to seven insecticides, namely, 3 organophosphate compounds (malathion, chlorpyrifos and pirimiphos-methyl), one carbamate (propoxur) and 1 pyrethroid (cypermethrin, deltamethrin and lambdacialotrine) of three field-collected strains of Blattella germanica (Linnaeus, 1767) from Santiago de Cuba.
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8551300 Mazzarri MB, Georghiou GP: Characterization of resistance to organophosphate, carbamate, and pyrethroid insecticides in field populations of Aedes aegypti from Venezuela. J Am Mosq Control Assoc. 1995 Sep;11(3):315-22.


Resistance to chlorpyrifos (OP), permethrin, and lambda-cyhalothrin (pyrethroids) was moderate (7-fold) in both populations.
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15659565 Carvajal F, Sanchez-Amate MC, Sanchez-Santed F, Cubero I: Neuroanatomical targets of the organophosphate chlorpyrifos by c-fos immunolabeling. Toxicol Sci. 2005 Apr;84(2):360-7. Epub 2005 Jan 19.

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17196233 Hancock S, Ehrich M, Hinckley J, Pung T, Jortner BS: The effect of stress on the acute neurotoxicity of the organophosphate insecticide chlorpyrifos. Toxicol Appl Pharmacol. 2007 Mar;219(2-3):136-41. Epub 2006 Nov 16.

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12143930 Varo I, Navarro JC, Amat F, Guilhermino L: Characterisation of cholinesterases and evaluation of the inhibitory potential of chlorpyrifos and dichlorvos to Artemia salina and Artemia parthenogenetica. Chemosphere. 2002 Aug;48(6):563-9.

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15802843 Thetkathuek A, Keifer M, Fungladda W, Kaewkungwal J, Padungtod C, Wilson B, Mankhetkorn S: Spectrophotometric determination of plasma and red blood cell cholinesterase activity of 53 fruit farm workers pre- and post-exposed chlorpyrifos for one fruit crop. Chem Pharm Bull. 2005 Apr;53(4):422-4.

We sought to investigate the early biological effects of chlorpyrifos among 53 Thai fruit farm workers by measuring the plasma cholinesterase (PChE) and red blood cell cholinesterase (AChE) activities, a biomarker of organophosphate (OPs) pesticide during one fruit crop.
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18468882 Teller C, Halamek J, Zeravik J, Stocklein WF, Scheller FW: Development of a bifunctional sensor using haptenized acetylcholinesterase and application for the detection of cocaine and organophosphates. Biosens Bioelectron. 2008 Sep 15;24(1):111-7. Epub 2008 Apr 1.

The organophosphate chlorpyrifos-oxon could be detected in concentrations from 10 (-6) down to 10 (-8) M after 20 min of injection time (equals to 500 microL sample volume.
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10677267 Dembele K, Haubruge E, Gaspar C: Concentration effects of selected insecticides on brain acetylcholinesterase in the common carp (Cyprinus carpio L.). Ecotoxicol Environ Saf. 2000 Jan;45(1):49-54.

Hence, in the present study in vivo exposure period effect and in vitro concentration-response of chlorfenvinphos, chlorpyrifos diazinon, and carbofuran were investigated on Cyprinus carpio L.
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17016712 Cardona D, Lopez-Grancha M, Lopez-Crespo G, Nieto-Escamez F, Sanchez-Santed F, Flores P: Vulnerability of long-term neurotoxicity of chlorpyrifos: effect on schedule-induced polydipsia and a delay discounting task. Psychopharmacology. 2006 Nov;189(1):47-57. Epub 2006 Oct 3.

The primary mechanism of acute toxic action of OPs is inhibition of acetylcholinesterase (AChE).
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9515941 Ehrich M, Correll L: Inhibition of carboxylesterases in SH-SY5Y human and NB41A3 mouse neuroblastoma cells by organophosphorus esters. J Toxicol Environ Health A. 1998 Mar 13;53(5):385-99.

CbxE are thought to protect the critical enzyme acetylcholinesterase (AChE) from OP inhibition in animals.
Therefore, this study examined concentration-related OP-induced inhibition of CbxE in human SH-SY5Y and mouse NB41A3 neuroblastoma cells with 11 active esterase inhibitors: paraoxon, malaoxon, chlorpyrifos-oxon, tolyl saligenin phosphate (TSP), phenyl saligenin phosphate (PSP), diisopropyl phosphorofluoridate (DFP), mipafox, dichlorvos, trichlorfon, dibutyryl dichlorovinyl phosphate (DBVP), and dioctyl dichlorovinyl phosphate (DOVP).
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17324631 Vioque-Fernandez A, de Almeida EA, Lopez-Barea J: Esterases as pesticide biomarkers in crayfish (Procambarus clarkii, Crustacea): tissue distribution, sensitivity to model compounds and recovery from inactivation. Comp Biochem Physiol C Toxicol Pharmacol. 2007 Apr;145(3):404-12. Epub 2007 Jan 30.

Since acetylcholinesterase prevails in nervous tissue and carboxylesterase in digestive gland, they are proposed as biomarkers.
Carboxylesterase was inhibited by carbaryl and chlorpyrifos, but not by eserine and malathion.
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16102564 Howard AS, Bucelli R, Jett DA, Bruun D, Yang D, Lein PJ: Chlorpyrifos exerts opposing effects on axonal and dendritic growth in primary neuronal cultures. Toxicol Appl Pharmacol. 2005 Sep 1;207(2):112-24.

In summary, these compounds perturb neuronal morphogenesis via opposing effects on axonal and dendritic growth, and both effects are independent of acetylcholinesterase inhibition.
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8722792 Bourguet D, Prout M, Raymond M: Dominance of insecticide resistance presents a plastic response. Genetics. 1996 May;143(1):407-16.

Dominance level of insecticide resistance provided by one major gene (an insensitive acetylcholinesterase) in the mosquito Culex pipiens was studied in two distinct environments.
Dominance level was found to be very different environments, varying from almost complete dominance to almost recessive when either propoxur (a carbamate insecticide) or chlorpyrifos (an organophosphorus insecticide) was used.
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