Protein Information

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

Compound Information

Name carbofuran
CAS

Reference List

PubMed Abstract RScore(About this table)
17804862 Zhang X, Tsang AM, Okino MS, Power FW, Knaak JB, Harrison LS, Dary CC: A physiologically based pharmacokinetic/pharmacodynamic model for carbofuran in Sprague-Dawley rats using the exposure-related dose estimating model. Toxicol Sci. 2007 Dec;100(2):345-59. Epub 2007 Sep 5.

Carbofuran (2,3-dihydro-2,2-dimethyl-7-benzofuranyl-N-methylcarbamate), a broad spectrum N-methyl carbamate insecticide, and its metabolite, 3-hydroxycarbofuran, exert their toxicity by reversibly inhibiting acetylcholinesterase (AChE).
175(2,2,4,5) Details
19287708 Pree DJ, Townshend JL, Cole KJ: Inhibition of Acetylcholinesterases from Aphelenchus avenae by Carbofuran and Fenamiphos. J Nematol. 1990 Apr;22(2):182-6.
169(2,2,3,4) Details
20112875 Tham LG, Perumal N, Syed MA, Shamaan NA, Shukor MY: Assessment of Clarias batrachus as a source of acetylcholinesterase (AchE) for the detection of insecticides. J Environ Biol. 2009 Jan;30(1):135-8.

Screening of insecticide and heavy metals showed that carbofuran and carbaryl strongly inhibited C. batrachus AChE.
166(2,2,2,6) Details
2778846 Gupta RC, Kadel WL: Prevention and antagonism of acute carbofuran intoxication by memantine and atropine. J Toxicol Environ Health. 1989;28(1):111-22.

A single sc dose of memantine HCl (MEM, 18 mg/kg) and atropine sulfate (ATS, 16 mg/kg) 60 and 15 min, respectively, prior to carbofuran administration completely prevented the expected gross toxic signs and significantly (p less than .01) attenuated the carbofuran-induced inhibition of AChE activity.
144(1,3,3,4) Details
3710030 Renzi BE, Krieger RI: Sublethal acute toxicity of carbosulfan [2,3-dihydro-2,2-dimethyl-7-benzofuranyl (d i-n-butylaminosulfenyl)(methyl) carbamate] in the rat after intravenous and oral exposures. Fundam Appl Toxicol. 1986 Jan;6(1):7-15.

Based on regression analysis and metabolic studies, both carbosulfan and carbofuran contributed to the observed AChE inhibition; however, carbofuran, a more potent in vitro inhibitor and the usual predominant inhibitor in plasma, was responsible for most of the erythrocyte AChE inhibition.
120(1,2,3,5) Details
17364237 Ahmed M, Rocha JB, Mazzanti CM, Morsch AL, Cargnelutti D, Correa M, Loro V, Morsch VM, Schetinger MR: Malathion, carbofuran and paraquat inhibit Bungarus sindanus (krait) venom acetylcholinesterase and human serum butyrylcholinesterase in vitro. Ecotoxicology. 2007 May;16(4):363-9. Epub 2007 Mar 16.
119(1,2,3,4) Details
16461013 Yi MQ, Liu HX, Shi XY, Liang P, Gao XW: Inhibitory effects of four carbamate insecticides on acetylcholinesterase of male and female Carassius auratus in vitro. Comp Biochem Physiol C Toxicol Pharmacol. 2006 May;143(1):113-6. Epub 2006 Feb 3.

The ratios of bimolecular rate constant (female/male) for AChE reacting with methomyl, thiodicarb, carbofuran and carbosulfan were 1.03, 2.44, 1.03 and 1.106, respectively.
117(1,2,2,7) Details
2033303 Ahmed YM: Kinetic study on inhibition of earthworm acetylcholinesterase by carbamate insecticides. J Egypt Soc Parasitol. 1991 Apr;21(1):283-92.

The inhibition progress of the AChE by aldicarb was relatively rapid more than the other two tested inhibitors: carbofuran and methomyl.
115(1,2,2,5) Details
16307259 Kamboj A, Kiran R, Sandhir R: Carbofuran-induced neurochemical and neurobehavioral alterations in rats: attenuation by N-acetylcysteine. Exp Brain Res. 2006 Apr;170(4):567-75. Epub 2005 Nov 24.

Acetylcholinesterase activity was significantly inhibited in all the regions of brain after carbofuran exposure (1 mg/kg body weight, orally, for 28 days).
87(1,1,2,2) Details
5076351 Yu CC, Metcalf RL, Booth GM: Inhibition of acetylcholinesterase from mammals and insects by carbofuran and its related compounds and their toxicities toward these animals. J Agric Food Chem. 1972 Sep-Oct;20(5):923-6.
81(1,1,1,1) Details
15450859 Damiens G, His E, Gnassia-Barelli M, Quiniou F, Romeo M: Evaluation of biomarkers in oyster larvae in natural and polluted conditions. Comp Biochem Physiol C Toxicol Pharmacol. 2004 Jun;138(2):121-8.

There was an inhibition of AChE activity with carbofuran, and a toxic effect shown by an increase in TBARS levels counteracted by increases in GST and CAT activities which protected the larvae.
84(1,1,1,4) Details
17166588 Forcella M, Berra E, Giacchini R, Rossaro B, Parenti P: Increased alanine concentration is associated with exposure to fenitrothion but not carbamates in Chironomus riparius larvae. Ecotoxicol Environ Saf. 2007 Mar;66(3):326-34. Epub 2006 Dec 12.

AChE activity was significantly reduced by all three insecticides, PNPAE by fenitrothion, carbofuran and carbaryl, whereas NAE activity was stimulated by carbaryl and unaffected by fenitrothion and carbofuran.
83(1,1,1,3) Details
19238297 Mukherjee J, Lumibao CY, Kirchhoff JR: Application of a thiol-specific electrocatalytic electrode for real-time amperometric monitoring of enzymatic hydrolysis. Analyst. 2009 Mar;134(3):582-6. Epub 2008 Dec 16.

The rapid and sensitive detection of thiocholine allowed monitoring the inhibition of acetylcholinesterase in the presence of the pesticide, carbofuran.
83(1,1,1,3) Details
9378096 Heath AG, Cech JJ Jr, Brink L, Moberg P, Zinkl JG: Physiological responses of fathead minnow larvae to rice pesticides. Ecotoxicol Environ Saf. 1997 Aug;37(3):280-8.

Acetylcholinesterase was reduced in those larvae exposed to the higher levels of carbofuran.
82(1,1,1,2) Details
8343977 Loewenstein Y, Denarie M, Zakut H, Soreq H: Molecular dissection of cholinesterase domains responsible for carbamate toxicity. Chem Biol Interact. 1993 Jun;87(1-3):209-16.

Comparative inhibition profiles were derived for five N-methyl carbamates, mostly carbofuran derivatives, differing in length and branching of their hydrocarbonic chain towards human erythrocyte acetylcholinesterase (H.AChE), human serum butyrylcholinesterase (H.BChE) in its normal form or in a mutant form containing the point mutation Asp70--> Gly, and Drosophila nervous system ChE.
82(1,1,1,2) 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
494273 Cambon C, Declume C, Derache R: Effect of the insecticidal carbamate derivatives (carbofuran, pirimicarb, aldicarb) on the activity of acetylcholinesterase in tissues from pregnant rats and fetuses. Toxicol Appl Pharmacol. 1979 Jun 30;49(2):203-8.
81(1,1,1,1) 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.
71(0,2,3,6) Details
15261450 Jarrard HE, Delaney KR, Kennedy CJ: Impacts of carbamate pesticides on olfactory neurophysiology and cholinesterase activity in coho salmon (Oncorhynchus kisutch). Aquat Toxicol. 2004 Aug 10;69(2):133-48.

All three carbamates also affected AChE activity levels in the OR and brain (BR): carbofuran exposure at 200 microg/l significantly inhibited AChE activity in the OR, and both IPBC and mancozeb significantly increased AChE activity in BR at multiple concentrations with acute localized exposure.
83(1,1,1,3) Details
2709439 Gupta RC, Kadel WL: Concerted role of carboxylesterases in the potentiation of carbofuran toxicity by iso-OMPA pretreatment. J Toxicol Environ Health. 1989;26(4):447-57.

Each drug when given alone (1.0 mg/kg iso-OMPA, 0.5 mg/kg carbofuran) caused a significant (p less than .01) inhibition of carboxylesterase (CarbE) activity in brain structures (cortex, stem, striatum, and hippocampus), skeletal muscle (hemidiaphragm), liver, and plasma, whereas acetylcholinesterase (AChE) activity remained significantly (p greater than .01) unchanged.
82(1,1,1,2) Details
18937214 Li H, Ricordel I, Tong L, Schopfer LM, Baud F, Megarbane B, Maury E, Masson P, Lockridge O: Carbofuran poisoning detected by mass spectrometry of butyrylcholinesterase adduct in human serum. J Appl Toxicol. 2009 Mar;29(2):149-55.

Carbofuran is a pesticide whose acute toxicity is due to inhibition of acetylcholinesterase.
81(1,1,1,1) Details
16931442 Kaur M, Sandhir R: Comparative effects of acute and chronic carbofuran exposure on oxidative stress and drug-metabolizing enzymes in liver. Drug Chem Toxicol. 2006;29(4):415-21.

Activity of acetylcholinesterase, a bona fide marker of carbofuran exposure, was markedly inhibited after acute carbofuran exposure, whereas the extent of inhibition was much less after chronic exposure.
81(1,1,1,1) Details
7123566 Mukhopadhyay PK, Mukherji AP, Dehadrai PV: Certain biochemical responses in the air-breathing catfish Clarias batrachus exposed to sublethal carbofuran. Toxicology. 1982;23(4):337-45.

Exposure to carbofuran resulted in sharp inhibition of acetylcholinesterase activity in brain of the fish which recovered rather rapidly after terminating pesticide treatment and maintaining the fish in clean freshwater.
81(1,1,1,1) Details
17724900 Gawlikowski T, Hubalewska-Dydejczyk A, Pach D: [Acute suicidal carbofuran poisoning--case report] . Przegl Lek. 2007;64(4-5):322-3.

The lowest activity of AChE was 0 IU/L.
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.
1(0,0,0,1) Details
16905305 Kim N, Park IS, Kim DK: High-sensitivity detection for model organophosphorus and carbamate pesticide with quartz crystal microbalance-precipitation sensor. Biosens Bioelectron. 2007 Mar 15;22(8):1593-9. Epub 2006 Aug 14.

When an inhibition study with the developed sensor was undertaken at the optimized AChE immobilization with varying concentrations of a model organophosphorus pesticide EPN and carbamate one carbofuran, a sensitive detection for them was possible with the limit of detection corresponding to 1.55 x 10 (-8) and 1.30 x 10 (-9) M, respectively.
32(0,1,1,2) Details
9592930 Keseru GM: [Application of theoretical and synthetic models to cytochrome P450 catalysed metabolic reactions]. Acta Pharm Hung. 1998 Mar;68(2):65-9.

Metabolism of an AChE inhibitor, carbofuran was studied.
31(0,1,1,1) Details
12485777 Ciucu AA, Negulescu C, Baldwin RP: Detection of pesticides using an amperometric biosensor based on ferophthalocyanine chemically modified carbon paste electrode and immobilized bienzymatic system. Biosens Bioelectron. 2003 Mar;18(2-3):303-10.

The method is based on a ferophthalocyanine chemically modified carbon paste electrode coupled with acetylcholinesterase and choline oxidase co-immobilized onto the surface of a dialysis membrane.
With this approach, up to 10 (-10) M of paraoxon and carbofuran can be detected.
1(0,0,0,1) Details
19277148 Gordon R, Chippett J, Tilley J: Effects of Two Carbamates on Infective Juveniles of Stemernema carpocapsae All Strain and Steinernema feltiae Umea Strain. J Nematol. 1996 Sep;28(3):310-7.

Laboratory bioassays were conducted to determine the effects of two carbamates, carbofuran (an acetylcholinesterase inhibitor) and fenoxycarb (a juvenile hormone analog), on survival and infectivity of the infective juveniles (IJ) of Steinernema feltiae Umea strain and Steinernema carpocapsae All strain.
31(0,1,1,1) Details
18340526 Kamboj SS, Kumar V, Kamboj A, Sandhir R: Mitochondrial oxidative stress and dysfunction in rat brain induced by carbofuran exposure. Cell Mol Neurobiol. 2008 Nov;28(7):961-9. Epub 2008 Mar 14.

There was a significant inhibition in the activity of acetylcholinesterase (66.6%) in brain samples after 28 days of carbofuran exposure.
31(0,1,1,1) Details
19107276 Llopis X, Pumera M, Alegret S, Merkoci A: Lab-on-a-chip for ultrasensitive detection of carbofuran by enzymatic inhibition with replacement of enzyme using magnetic beads. Lab Chip. 2009 Jan 21;9(2):213-8. Epub 2008 Dec 1.

In this paper an ultrasensitive method to determine toxicity due to pesticides in a glass lab-on-a-chip by means of enzymatic inhibition of acetylcholinesterase immobilised on magnetic beads is described.
1(0,0,0,1) Details
15568361 Wu G, Jiang S, Miyata T: Seasonal changes of methamidophos susceptibility and biochemical properties in Plutella xylostella (Lepidoptera: Yponomeutidae) and its parasitoid Cotesia plutellae (Hymenoptera: Braconidae). J Econ Entomol. 2004 Oct;97(5):1689-98.

Methamidophos resistance and acetylcholinesterase (AChE) insensitivity to methamidophos, dichlorvos, and carbofuran were determined in the field populations of Plutella xylostella (L.) (Lepidoptera: Yponomeutidae) and its parasitoid Cotesia plutellae Kurdjumov (Hymenoptera: Braconidae) collected from the corresponding hosts between October 1998 and December 2003 in Fuzhou and Minhou, Fijian, China.
23(0,0,3,8) Details
18663432 Valdes-Ramirez G, Cortina M, Ramirez-Silva MT, Marty JL: Acetylcholinesterase-based biosensors for quantification of carbofuran, carbaryl, methylparaoxon, and dichlorvos in 5% acetonitrile. Anal Bioanal Chem. 2008 Oct;392(4):699-707. Epub 2008 Jul 29.
19(0,0,3,4) Details
19449386 Anguiano GA, Amador A, Moreno-Legorreta M, Arcos-Ortega F, Vazquez-Boucard C: Effects of exposure to oxamyl, carbofuran, dichlorvos, and lindane on acetylcholinesterase activity in the gills of the Pacific oyster Crassostrea gigas. Environ Toxicol. 2009 May 15.
16(0,0,2,6) Details
15664429 Milatovic D, Gupta RC, Dekundy A, Montine TJ, Dettbarn WD: Carbofuran-induced oxidative stress in slow and fast skeletal muscles: prevention by memantine and atropine. Toxicology. 2005 Mar 1;208(1):13-24.

Acute toxic effects of acetylcholinesterase (AChE) inhibitors on skeletal muscles are thought to involve oxidative stress with increased generation of free radicals such as reactive oxygen species (ROS) and reactive nitrogen species (RNS).
1(0,0,0,1) Details
16897762 Lotti M, Moretto A: Do carbamates cause polyneuropathy? . Muscle Nerve. 2006 Oct;34(4):499-502.


Carbamates are reversible inhibitors of acetylcholinesterase, and some also inhibit neuropathy target esterase (NTE), the target in organophosphate-induced delayed polyneuropathy.
1(0,0,0,1) Details
17673351 Zeljezic D, Vrdoljak AL, Radic B, Fuchs N, Berend S, Orescanin V, Kopjar N: Comparative evaluation of acetylcholinesterase status and genome damage in blood cells of industrial workers exposed to carbofuran. Food Chem Toxicol. 2007 Dec;45(12):2488-98. Epub 2007 Jun 21.
10(0,0,1,5) Details
19856836 Podolska M: [Anisakis simplex larvae from the Baltic herring as tag organisms in biological and fisheries research. Wiad Parazytol. 2009;55(3):211-7.

Acetylcholinesterase (AChE) activity in the tissues of host and the parasite and the impact of carbofuran, a carbamate pesticide on the AChE activity in A. simplex larvae was investigated.
7(0,0,1,2) Details
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.
1(0,0,0,1) Details
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.
1(0,0,0,1) Details
16257038 Romeo M, Gharbi-Bouraoui S, Gnassia-Barelli M, Dellali M, Aissa P: Responses of Hexaplex (Murex) trunculus to selected pollutants. Sci Total Environ. 2006 Apr 15;359(1-3):135-44. Epub 2005 Oct 27.

An evaluation of the biological effects of the most toxic metals (cadmium and copper) and of two organics (carbofuran and lindane), present in the sediments of the Bizerta lagoon, was attempted by measuring biomarkers (acetylcholinesterase: AChE, catalase: CAT and glutathione S-transferase: GST activities) in animals experimentally exposed for 48 or 72 h.
13(0,0,2,3) Details
11993279 Pogacnik L, Franko M: Validation of different commercially available cholinesterases for pesticide toxicity test. Ann Chim. 2002 Jan-Feb;92(1-2):93-101.

A systematic study of different commercially available cholinesterases (AChEs from electric eel, human erythrocytes, bovine erythrocytes and BuChE from horse serum) for the FIA determination of some frequently used organophosphate (paraoxon, oxydemeton-methyl, triazophos, diazionon) and carbamate (carbofuran, propoxur) pesticides was carried out.
7(0,0,1,2) Details
10353999 Dembele K, Haubruge E, Gaspar C: Recovery of acetylcholinesterase activity in the common carp (Cyprinus carpio L.) after inhibition by organophosphate and carbamate compounds. Bull Environ Contam Toxicol. 1999 Jun;62(6):731-42.

1(0,0,0,1) Details
4139992 Karnak RE, Collins WJ: The susceptibility to selected insecticides and acetylcholinesterase activity in a laboratory colony of midge larvae, Chironomus tentans (diptera: chironomidae). Bull Environ Contam Toxicol. 1974 Jul;12(1):62-9.

1(0,0,0,1) Details
2322020 Hussain M, Yoshida K, Atiemo M, Johnston D: Occupational exposure of grain farmers to carbofuran. . Arch Environ Contam Toxicol. 1990 Mar-Apr;19(2):197-204.

Blood samples were analyzed for acetylcholinesterase (AChE), pseudocholinesterase (ChE) and several other blood parameters.
1(0,0,0,1) Details
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.
7(0,0,0,7) Details
15297019 Lee BW, Oh SH, Chung JH, Moon CK, Lee BH: N-nitroso metabolite of carbofuran induces apoptosis in CHL cells by cytochrome c-mediated activation of caspases. Toxicology. 2004 Sep 1;201(1-3):51-8.

Carbofuran is an anti-acetylcholinesterase insecticide regarded as a relatively safe chemical based on extensive toxicological data.
6(0,0,1,1) Details
1595894 Kumaran S, Tran-Minh C: Determination of organophosphorous and carbamate insecticides by flow injection analysis. Anal Biochem. 1992 Jan;200(1):187-94.

A flow injection system, incorporating an acetylcholinesterase (AChE) single bead string reactor (SBSR), for the determination of some organophosphorous (azinphos-ethyl, azinphos-methyl, bromophos-methyl, dichlorovos, fenitrothion, malathion, paraoxon, parathion-ethyl and parathion-methyl) and carbamate insecticides (carbofuran and carbaryl) is presented.
6(0,0,1,1) Details
18965297 Quintero MC, Silva M, Perez-Bendito D: Enzymatic determination of N-methylcarbamate pesticides at the nanomolar level by the stopped-flow technique. Talanta. 1991 Nov;38(11):1273-7.

It is based on their inhibitory effect on electric eel acetylcholinesterase and the use of 5,5'-dithiobis (2-nitrobenzoic) acid (DTNB) as chromogenic reagent for the thiocholine released from the acetylthiocholine iodide substrate.
Carbaryl, propoxur and carbofuran can be determined at concentrations in the ranges 6.5-120, 2-15 and 0.1-5.0 ng/ml, respectively, by the proposed method.
1(0,0,0,1) Details
11286337 Bachmann TT, Leca B, Vilatte F, Marty JL, Fournier D, Schmid RD: Improved multianalyte detection of organophosphates and carbamates with disposable multielectrode biosensors using recombinant mutants of Drosophila acetylcholinesterase and artificial neural networks. Biosens Bioelectron. 2000 Jun;15(3-4):193-201.

Multisensors I and II were both used for inhibition analysis of binary paraoxon and carbofuran mixtures in a concentration range 0-5 microg/l, followed by data analysis using feed-forward ANN.
6(0,0,0,6) Details
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.
6(0,0,0,6) Details
16268118 Rendon von Osten J, Epomex C, Tinoco-Ojanguren R, Soares AM, Guilhermino L: Effect of pesticide exposure on acetylcholinesterase activity in subsistence farmers from Campeche, Mexico. Arch Environ Health. 2004 Aug;59(8):418-25.

Carbamates, particularly carbofuran, seem to be more associated with exuberant and diversified symptomatology of pesticide exposure than organophosphates.
5(0,0,0,5) Details
19934164 Moser VC, McDaniel KL, Phillips PM, Lowit AB: Time-course, dose-response, and age comparative sensitivity of N-methyl carbamates in rats. Toxicol Sci. 2010 Mar;114(1):113-23. Epub 2009 Nov 24.

N-Methyl carbamate insecticides are reversible inhibitors of central and peripheral acetylcholinesterase (ChE).
To study potential age-related differences, we evaluated seven carbamates (carbaryl, carbofuran, formetanate, methiocarb, methomyl, oxamyl, and propoxur) in preweanling (17 days old or postnatal day [PND] 17) male rats.
1(0,0,0,1) Details
9478101 Lata S, Janiszewski J, Madej T: Accidental oral poisoning with carbamate in a 26-year-old patient. Przegl Lek. 1997;54(10):753-5.

Acute, accidental, oral poisoning with carbofuran in a chronic alcoholic was presented.
Toxicological examination revealed non acetylcholinesterase activity.
1(0,0,0,1) Details
15362815 Wobeser G, Bollinger T, Leighton FA, Blakley B, Mineau P: Secondary poisoning of eagles following intentional poisoning of coyotes with anticholinesterase pesticides in western Canada. J Wildl Dis. 2004 Apr;40(2):163-72.

Carbofuran was identified in nine incidents.
The diagnosis was confirmed in eight instances by demonstration of pesticide in ingesta from eagles or known use of pesticide at the site together with brain cholinesterase (AChE) reduction of > 50% in at least one animal.
4(0,0,0,4) Details
9371089 Vaughan A, Rocheleau T, ffrench-Constant R: Site-directed mutagenesis of an acetylcholinesterase gene from the yellow fever mosquito Aedes aegypti confers insecticide insensitivity. Exp Parasitol. 1997 Nov;87(3):237-44.

4(0,0,0,4) Details
10918524 Gupta RC, Goad JT, Milatovic D, Dettbarn WD: Cholinergic and noncholinergic brain biomarkers of insecticide exposure and effects. Hum Exp Toxicol. 2000 May;19(5):297-308.

The objective of this investigation was to determine the distribution of cholinergic and noncholinergic biomarkers in discrete brain regions (cortex, stem, striatum, hippocampus, and cerebellum) of rats treated with dimethyl sulfoxide (DMSO, controls), and insecticides such as carbofuran (CARB, 1.5 mg/kg, sc), or methyl parathion (MPTH, 5 mg/kg, ip).
In controls, analyses of the brain regions revealed a wide variability in the values of cholinergic (acetylcholinesterase, AChE) and noncholinergic (creatine kinase, CK; and lactic dehydrogenase, LDH, and their isoenzymes) biomarkers.
4(0,0,0,4) Details
7447699 Cambon C, Declume C, Derache R: Foetal and maternal rat brain acetylcholinesterase: isoenzymes changes following insecticidal carbamate derivatives poisoning. Arch Toxicol. 1980 Oct;45(4):257-62.

Pregnant rats (18th day) were orally given insecticidal carbamates with anticholinesterasic properties: 50 mg/kg carbaryl, 0.1 mg/kg aldicarb, 2.5 mg/kg carbofuran and 20 mg/kg pirimicarb.
3(0,0,0,3) Details
16197955 Fabel S, Niessner R, Weller MG: Effect-directed analysis by high-performance liquid chromatography with gas-segmented enzyme inhibition. J Chromatogr A. 2005 Dec 16;1099(1-2):103-10. Epub 2005 Sep 28.

A reversed-phase high-performance liquid chromatography system with UV-detector was equipped with an on-line acetylcholinesterase inhibition assay to achieve effect-directed analysis of potentially toxic samples.
The limit of detection of two model compounds carbofuran (carbamate) and paraoxon-ethyl (organophosphate) was determined to be 13 ng (injected mass) and 7.4 ng, respectively, applying an isocratic chromatography method.
1(0,0,0,1) Details
18966870 Andres RT, Narayanaswamy R: Fibre-optic pesticide biosensor based on covalently immobilized acetylcholinesterase and thymol blue. Talanta. 1997 Aug;44(8):1335-52.

Inhibition plots obtained for test organophosphate (paraoxon) and carbamate (carbofuran) pesticides exhibited concentration-dependent behaviour and showed linear profiles in the concentration ranges 5x10 (-8)-5x10 (-7) M for carbofuran and 5x10 (-7)-5x10 (-6) M for paraoxon.
3(0,0,0,3) Details
8239714 Heath AG, Cech JJ Jr, Zinkl JG, Steele MD: Sublethal effects of three pesticides on Japanese medaka. Arch Environ Contam Toxicol. 1993 Nov;25(4):485-91.

One- to 2-day-old medaka (Oryzias latipes) larvae were exposed for 4 days to the rice field pesticides methyl parathion, molinate, carbofuran and a mixture of all three.
Maximum swimming speed, spontaneous muscular activity, acetylcholinesterase activity, dry weight, RNA:DNA ratio, and five morphometric variables were determined at the end of the exposures.
3(0,0,0,3) Details
8343987 Gupta RC, Dettbarn WD: Role of carboxylesterases in the prevention and potentiation of N-methylcarbamate toxicity. Chem Biol Interact. 1993 Jun;87(1-3):295-303.

Pretreatment of rats with iso-OMPA one hour prior to each of the N-methylcarbamate insecticides, carbofuran, propoxur, or aldicarb, potentiated the toxicity of these carbamates threefold.
None of these compounds alone in the dosage used produced toxic signs; however, carboxylesterase (CarbE) activity in a variety of organs including brain, muscle, liver, and plasma was significantly reduced, while acetylcholinesterase (AChE) activity was unchanged.
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18968286 Pogacnik L, Franko M: Optimisation of FIA system for detection of organophosphorus and carbamate pesticides based on cholinesterase inhibition. Talanta. 2001 May 30;54(4):631-41.

The sensitivity of the bioanalytical FIA system containing different immobilised cholinesterases (AChEs from electric eel, human erythrocytes, bovine erythrocytes and BuChE from horse serum) for determination of organophosphorus and carbamate pesticides was tested.
Responses to some frequently used organophosphorus (paraoxon, oxydemeton-methyl, triazophos) and carbamate (carbofuran, propoxur) pesticides were found to be dependent on the origin of cholinesterases.
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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.
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16076434 Suwansa-ard S, Kanatharana P, Asawatreratanakul P, Limsakul C, Wongkittisuksa B, Thavarungkul P: Semi disposable reactor biosensors for detecting carbamate pesticides in water. Biosens Bioelectron. 2005 Sep 15;21(3):445-54. Epub 2004 Dec 21.

Acetylcholinesterase was immobilized on silica gel by covalent binding. pH and conductivity electrodes were used to detect the ionic change of the sample solution due to hydrolysis of acetylcholine.
Carbofuran and carbaryl were used to test these systems.
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6693000 Ferguson PW, Dey MS, Jewell SA, Krieger RI: Carbofuran metabolism and toxicity in the rat. Fundam Appl Toxicol. 1984 Feb;4(1):14-21.

The influence of carbofuran metabolism on acetylcholinesterase inhibition has been defined after low dose (50 micrograms/kg, iv and oral) [carbonyl-14C] carbofuran exposures to male Sprague-Dawley rats.
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14761699 Panda S, Sahu SK: Recovery of acetylcholine esterase activity of Drawida willsi (Oligochaeta) following application of three pesticides to soil. Chemosphere. 2004 Apr;55(2):283-90.

A sharp decline in the AChE activity of D. willsi was observed up to 9 and 12 days following treatment of carbofuran and malathion in both single and double doses, respectively, whereas very little inhibition was noticed in case of butachlor.
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11023689 Bretaud S, Toutant JP, Saglio P: Effects of carbofuran, diuron, and nicosulfuron on acetylcholinesterase activity in goldfish (Carassius auratus). Ecotoxicol Environ Saf. 2000 Oct;47(2):117-24.

In brain, AChE activity was significantly inhibited during all the periods of exposure in response to 50 microg/L (19-28%) and 500 microg/L (85-87%) carbofuran.
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6710541 Gupta M, Bagchi GK, Gupta SD, Sasmal D, Chatterjee T, Dey SN: Changes of acetylcholine, catecholamines and amino acid in mice brain following treatment with Nuvacron and Furadan. Toxicology. 1984 Mar;30(2):171-5.


The following were measured: acetylcholine, acetylcholinesterase, gamma-aminobutyric acid, epinephrine, norepinephrine, dopamine and 5-hydroxytryptamine.
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11570692 Gupta RC, Milatovic D, Dettbarn WD: Nitric oxide modulates high-energy phosphates in brain regions of rats intoxicated with diisopropylphosphorofluoridate or carbofuran: prevention by N-tert-butyl-alpha-phenylnitrone or vitamin E. Arch Toxicol. 2001 Aug;75(6):346-56.

With either acetylcholinesterase (AChE) inhibitor, the maximum increase in citrulline levels was noted 30 min post-injection (> 6- to 7-fold in the cortex, and > 3- to 4-fold in the amygdala or hippocampus).
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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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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.
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14709383 Kok FN, Hasirci V: Determination of binary pesticide mixtures by an acetylcholinesterase-choline oxidase biosensor. Biosens Bioelectron. 2004 Feb 15;19(7):661-5.

Enzyme immobilized membrane was used in the detection of anti-cholinesterase activity of aldicarb (AS), carbofuran (CF) and carbaryl (CL), as well as two mixtures, (AS+CF) and (AS+CL).
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15532677 Benting J, Nauen R: Biochemical evidence that an S431F mutation in acetylcholinesterase-1 of Aphis gossypii mediates resistance to pirimicarb and omethoate. Pest Manag Sci. 2004 Nov;60(11):1051-5.

Here, we describe for the first time that recombinantly expressed AChE1 from A gossypii carrying the S431F mutation is insensitive to pirimicarb and omethoate, but sensitive to demeton-S-methyl and hypersensitive to carbofuran.
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7966439 Gupta RC, Goad JT, Kadel WL: Cholinergic and noncholinergic changes in skeletal muscles by carbofuran and methyl parathion. J Toxicol Environ Health. 1994 Nov;43(3):291-304.

The objective of this investigation was to determine the distribution of cholinergic (acetyl-cholinesterase, AChE) and noncholinergic markers in slow-, fast-, and mixed-fiber containing muscles (soleus, SOL; extensor digitorum longus, EDL; and diaphragm, DIA, respectively).
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17188316 Gupta RC, Milatovic S, Dettbarn WD, Aschner M, Milatovic D: Neuronal oxidative injury and dendritic damage induced by carbofuran: protection by memantine. Toxicol Appl Pharmacol. 2007 Mar;219(2-3):97-105. Epub 2006 Nov 1.

Pretreatment with the N-methyl-D-aspartate (NMDA) receptor antagonist memantine (18 mg/kg, sc), in combination with atropine sulfate (16 mg/kg, sc), significantly attenuated carbofuran-induced changes in AChE activity and levels of F (2)-IsoPs and F (4)-NeuroPs, declines in HEPs, as well as the alterations in morphology of hippocampal neurons.
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16023954 Chouteau C, Dzyadevych S, Durrieu C, Chovelon JM: A bi-enzymatic whole cell conductometric biosensor for heavy metal ions and pesticides detection in water samples. Biosens Bioelectron. 2005 Aug 15;21(2):273-81. Epub 2004 Dec 8.

For pesticides, first experiments showed that paraoxon-methyl inhibits C. vulgaris AChE contrary to parathion-methyl and carbofuran.
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9216867 Kallander DB, Fisher SW, Lydy MJ: Recovery following pulsed exposure to organophosphorus and carbamate insecticides in the midge, Chironomus riparius. Arch Environ Contam Toxicol. 1997 Jul;33(1):29-33.

The importance of recovery following pulsed and continuous exposure was determined by measuring the acute toxicity of two organophosphorus (parathion and malathion) and four carbamate (aldicarb, carbaryl, carbofuran and propoxur) insecticides.
Acetylcholinesterase activity in midges given two 1-h pulses of carbaryl separated by 24 h in clean water showed reactivation to control levels between the two exposures.
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16518518 Milatovic D, Gupta RC, Aschner M: Anticholinesterase toxicity and oxidative stress. ScientificWorldJournal. 2006 Feb 28;6:295-310.

Pretreatment with N-methyl D-aspartate (NMDA) receptor antagonist memantine, in combination with atropine sulfate, provides significant protection against inhibition of AChE, increases of ROS/RNS, and depletion of high-energy phosphates induced by DFP/carbofuran.
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19733130 Qu Y, Sun Q, Xiao F, Shi G, Jin L: Layer-by-Layer self-assembled acetylcholinesterase/PAMAM-Au on CNTs modified electrode for sensing pesticides. Bioelectrochemistry. 2010 Feb;77(2):139-44. Epub 2009 Aug 12.

In this paper, an acetylcholinesterase (AChE)/dendrimers polyamidoamine (PAMAM)-Au/Carbon nanotubes (CNTs) multilayer modified electrode based on LbL self-assembled technique was employed in the detection of carbofuran in samples.
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3268109 Guhathakurta S, Bhattacharya S: Target and nontarget actions of phenthoate and carbofuran: brain acetylcholinesterase, kidney iodide peroxidase, and blood thyroxine profiles in Channa punctatus. Biomed Environ Sci. 1988 Jun;1(1):59-63.

These xenobiotics caused significant inhibition of brain acetylcholinesterase concomitant with low kidney iodide peroxidase activity and depressed blood thyroxine levels.
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11131904 Katsoudas E, Abdelmesseh HH: Enzyme inhibition and enzyme-linked immunosorbent assay methods for carbamate pesticide residue analysis in fresh produce. J Food Prot. 2000 Dec;63(12):1758-60.

An acetylcholinesterase inhibition method was employed for detection of 21 carbamate pesticides in bananas, peaches, strawberries, and tomatoes.
The detection levels ranged from 0.1 ppm for carbofuran and 3-hydroxycarbofuran to 6 ppm for promecarb and aldicarb sulfoxide.
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11405258 Gupta RC, Milatovic D, Dettbarn WD: Depletion of energy metabolites following acetylcholinesterase inhibitor-induced status epilepticus: protection by antioxidants. Neurotoxicology. 2001 Apr;22(2):271-82.

In rats, SE was induced by either of two inhibitors of acetylcholinesterase (AChE), the organophosphate diisopropylphosphorofluoridate (DFP, 1.25 mg/kg, sc)- or the carbamate carbofuran (1.25 mg/kg, sc).
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15951093 Senger MR, Rico EP, de Bem Arizi M, Rosemberg DB, Dias RD, Bogo MR, Bonan CD: Carbofuran and malathion inhibit nucleotide hydrolysis in zebrafish (Danio rerio) brain membranes. Toxicology. 2005 Sep 1;212(2-3):107-15.

Since acetylcholine and ATP are co-released at the synapse and the acetylcholinesterase inhibition is an important target for pesticide action, here we verified the effect of exposure in vitro and in vivo to carbofuran and malathion on ectonucleotidase activities from brain membranes of zebrafish.
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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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1958080 Gupta RC, Goad JT, Kadel WL: In vivo alterations in lactate dehydrogenase (LDH) and LDH isoenzymes patterns by acute carbofuran intoxication. Arch Environ Contam Toxicol. 1991 Aug;21(2):263-9.

These alterations in LDH and its isoenzymes, in addition to acetylcholinesterase inhibition, may be directly or indirectly related to the mechanism (s) of the toxic action, and also provide insight into the site/organ (s) of toxic injury, thus providing an early prognostic indicator.
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