Protein Information

Name anticholinesterase
Synonyms Acylcholine acylhydrolase; BCHE; BCHE protein; Butyrylcholine esterase; Butyrylcholinesterase; CHE1; Choline esterase II; Cholinesterase…

Compound Information

Name aldicarb
CAS

Reference List

PubMed Abstract RScore(About this table)
9931232 Sturm A, Hansen P: Altered cholinesterase and monooxygenase levels in Daphnia magna and Chironomus riparius exposed to environmental pollutants. Ecotoxicol Environ Saf. 1999 Jan;42(1):9-15.

Parathion, dichlorvos, and aldicarb caused dose-related inhibition of cholinesterase (ChE) in 24-h bioassays with both species.
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11029035 Pilon M, Peng XR, Spence AM, Plasterk RH, Dosch HM: The diabetes autoantigen ICA69 and its Caenorhabditis elegans homologue, ric-19, are conserved regulators of neuroendocrine secretion. Mol Biol Cell. 2000 Oct;11(10):3277-88.

On the basis of the aldicarb resistance phenotype, we named the gene ric-19 (resistance to inhibitors of cholinesterase-19).
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12151634 El-Alfy AT, Schlenk D: Effect of 17beta-estradiol and testosterone on the expression of flavin-containing monooxygenase and the toxicity of aldicarb to Japanese medaka, Oryzias latipes. Toxicol Sci. 2002 Aug;68(2):381-8.

Since aldicarb acts by inhibiting the enzyme cholinesterase (ChE), the effect of sex hormones on the activity of this enzyme was also examined.
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11719702 Wang J, Grisle S, Schlenk D: Effects of salinity on aldicarb toxicity in juvenile rainbow trout (Oncorhynchus mykiss) and striped bass (Morone saxatilis x chrysops). Toxicol Sci. 2001 Dec;64(2):200-7.

These results suggest that salinity-mediated enhancement of aldicarb toxicity is species-dependent, and at least partially due to the salinity-related upregulation of FMOs, which, in turn, increases the bioactivation of aldicarb to aldicarb sulfoxide, which is a more potent inhibitor of cholinesterase than aldicarb.
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14979094 Costa C, Catania S, Silvari V: [Genotoxicity and activation of organophosphate and carbamate pesticides by cytochrome P450 2D6]. G Ital Med Lav Ergon. 2003 Jul-Sep;25 Suppl(3):81-2.

The role of the polymorphic cytochrome P450 (CYP) 2D6 isoform in catalysing the oxidative biotransformation of the organophosphate pesticide chlorpyriphos and the carbamate aldicarb into structures that inhibit cholinesterase and induce genotoxicity has been investigated in microsomal fraction, using quinine as a specific chemical inhibitor of CYP 2D6.
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11786345 Ivanov AN, Lukachova LV, Evtugyn GA, Karyakina EE, Kiseleva SG, Budnikov HC, Orlov AV, Karpacheva GP, Karyakin AA: Polyaniline-modified cholinesterase sensor for pesticide determination. Bioelectrochemistry. 2002 Jan;55(1-2):75-7.

The detection limits found (coumaphos, 0.002, trichlorfon, 0.04, aldicarb, 0.03, methiocarb, 0.08 mg l (-1)) make it possible to detect the pollutants in the waters on the level of limited threshold levels without sample preconcentration.
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17292441 Kuster E, Altenburger R: Suborganismic and organismic effects of aldicarb and its metabolite aldicarb-sulfoxide to the zebrafish embryo (Danio rerio). Chemosphere. 2007 Jun;68(4):751-60. Epub 2007 Feb 9.

In addition, suborganismic effects were examined analysing the enzyme inhibition of cholinesterases and carboxylesterases.
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17931764 Grauer E, Levy A: Oxotremorine-induced hypothermia as a method for evaluating long-term neuronal changes following poisoning by cholinesterase inhibitors in rats. Toxicology. 2007 Dec 5;242(1-3):1-6. Epub 2007 Sep 5.

One month after exposure to approximately 1LD (50) of the carbamates aldicarb and oxamyl, the hypothermic effect of oxotremorine was similar to that found in saline-treated control group.
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8285817 Burgess JL, Bernstein JN, Hurlbut K: Aldicarb poisoning. Arch Intern Med. 1994 Jan 24;154(2):221-4.

A case report with prolonged cholinesterase inhibition and improvement after pralidoxime therapy..
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4078930 DePass LR, Weaver EV, Mirro EJ: Aldicarb sulfoxide/aldicarb sulfone mixture in drinking water of rats: effects on growth and acetylcholinesterase activity. J Toxicol Environ Health. 1985;16(2):163-72.

Blood was collected after 8, 15, and 29 d of treatment for plasma and erythrocyte cholinesterase determinations, and brain cholinesterase was determined at sacrifice.
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1554768 Dorman DC, Harlin KA, Haschek WM, Ross SS, Wisse CA, Meerdink GL: Aldicarb toxicosis in a flock of sheep. J Vet Diagn Invest. 1992 Jan;4(1):45-7.

Inhibition of cholinesterase activity in retina (21.2-68.1% of normal activity, n = 3), brain (40.6-45.6% of normal activity, n = 3), and whole blood (27% of normal activity, n = 1) supported a diagnosis of carbamate toxicosis.
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6510327 Hill EF, Camardese MB: Toxicity of anticholinesterase insecticides to birds: technical grade versus granular formulations. Ecotoxicol Environ Saf. 1984 Dec;8(6):551-63.

The test chemicals were Amaze 15G (isofenphos), Counter 15G (terbufos), Dasanit 15G (fensulfothion), Diazinon 14G (diazinon), Di-Syston 15G (disulfoton), Dyfonate 20G (fonofos), Furadan 10G (carbofuran), Lorsban 15G (chlorpyrifos), Nemacur 15G (fenamiphos), Parathion 10G (parathion), Tattoo 10G (bendiocarb), Temik 15G (aldicarb), and Thimet 15G (phorate).
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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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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.

A growing body of evidence indicates that young animals exhibit an increased susceptibility to the lethal effects of cholinesterase (ChE)-inhibiting insecticides.
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.
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10871426 Parker ML, Goldstein MI: Differential toxicities of organophosphate and carbamate insecticides in the nestling European starling (Sturnus vulgaris). Arch Environ Contam Toxicol. 2000 Aug;39(2):233-42.

The concept of B-esterase buffering against anti-cholinesterase (ChE) insecticide toxicity has been extensively researched in mammalian species.
We quantified B-esterase buffering of organophosphate (diazinon and methyl parathion) and carbamate (aldicarb and oxamyl) toxicity in nestling European starlings (Sturnus vulgaris).
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8349949 Casale GP, Vennerstrom JL, Bavari S, Wang TL: Inhibition of interleukin 2 driven proliferation of mouse CTLL2 cells, by selected carbamate and organophosphate insecticides and congeners of carbaryl. Immunopharmacol Immunotoxicol. 1993 Mar-Jun;15(2-3):199-215.

The anticholinesterase (antiCHE) insecticides, a large family of pesticides used extensively throughout the world, inhibit serine hydrolases by carbamylating or phosphorylating a serine residue at the catalytic site.
The order of potency for T cell inhibition was carbaryl = dichlorvos > methiocarb > carbofuran > paraoxon > mevinphos > aldicarb = monocrotophos.
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8901627 Miller KG, Alfonso A, Nguyen M, Crowell JA, Johnson CD, Rand JB: A genetic selection for Caenorhabditis elegans synaptic transmission mutants. Proc Natl Acad Sci U S A. 1996 Oct 29;93(22):12593-8.


We have isolated 165 Caenorhabditis elegans mutants, representing 21 genes, that are resistant to inhibitors of cholinesterase (Ric mutants).
1(0,0,0,1) Details
10366542 Moser VC: Comparison of aldicarb and methamidophos neurotoxicity at different ages in the rat: behavioral and biochemical parameters. Toxicol Appl Pharmacol. 1999 Jun 1;157(2):94-106.

The neurotoxic effects of cholinesterase (ChE)-inhibiting pesticides are of particular concern for human health risk assessment due to the widespread exposure potential in children.
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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).
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18436673 Berny P, Gaillet JR: Acute poisoning of Red Kites (Milvus milvus) in France: data from the Sagir network. J Wildl Dis. 2008 Apr;44(2):417-26.

The major toxicants found were cholinesterase inhibitors (carbamates and organophosphate insecticides) and anticoagulant compounds.
The circumstances of exposure include secondary poisoning after the use of anticoagulants over vast areas to control water vole (Arvicola terrestric) populations, but they also include malicious poisoning with carbamates (aldicarb and cabofuran) in meat baits.
1(0,0,0,1) Details
9022648 Lifshitz M, Shahak E, Bolotin A, Sofer S: Carbamate poisoning in early childhood and in adults. J Toxicol Clin Toxicol. 1997;35(1):25-7.

The ingested poisons in all cases were positively identified as methomyl or aldicarb by gas chromatography-mass spectrometry.
RESULTS: Symptoms of intoxication in children were compared to those in adults with similar depression of the serum cholinesterase.
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8163760 Moritz F, Droy JM, Dutheil G, Melki J, Bonmarchand G, Leroy J: Acute pancreatitis after carbamate insecticide intoxication. Intensive Care Med. 1994;20(1):49-50.

A 29-year-old woman was admitted to the Rouen University Hospital for attempted suicide by ingestion of a carbamate insecticide (Temik G, containing 10% aldicarb).
Pseudocholinesterase levels took 77 days to return to normal.
1(0,0,0,1) Details
8134223 Lifshitz M, Rotenberg M, Sofer S, Tamiri T, Shahak E, Almog S: Carbamate poisoning and oxime treatment in children: a clinical and laboratory study. Pediatrics. 1994 Apr;93(4):652-5.

OBJECTIVE: (1) Retrospective evaluation of the clinical course of carbamate poisoning and the effect of oxime therapy in children. (2) In vitro study of the effect of oximes on the reactivation of carbamylated cholinesterase.
The poisoning agents in all cases were positively identified as methomyl or aldicarb by gas chromatography-mass spectrometry. (2) Laboratory study: The direct effect of obidoxime and of pralidoxime on acetylcholinesterase activity in vitro was investigated in normal human packed red blood cells pretreated with an organophosphate (paraoxon) or a carbamate (aldicarb or methomyl).
1(0,0,0,1) Details
3508476 Mansour NA, Valdes JJ, Shamoo AE, Annau Z: Biochemical interactions of carbamates and ecothiophate with the activated conformation of nicotinic acetylcholine receptor. J Biochem Toxicol. 1987 Spring;2:25-42.

While we observed a high potency of Neo and Physo in inhibiting [125-I]-alpha-BGT binding, it was undetectable for the carbamate insecticide 2-methyl-2-(methylthio) propionaldehyde-O-(methylcarbamoyl) oxime (aldicarb).
These data suggest that the potent anticholinesterase carbamate agents interact differently with the AChR and its ionic channel.
1(0,0,0,1) Details
9185888 Dourson ML, Teuschler LK, Durkin PR, Stiteler WM: Categorical regression of toxicity data: a case study using aldicarb. . Regul Toxicol Pharmacol. 1997 Apr;25(2):121-9.

When blood cholinesterase inhibition of 20% or more is considered as an adverse effect, a maximum likelihood risk estimate of adverse effects is 0.1% at a dose 10-fold higher than the RfD.
1(0,0,0,1) Details
406567 Schmid ER, Damboritz W, Markl P: [Radiometric determination of 11 carbamate pesticides in the nanogram and subnanongram ranges by means of cholinesterase inhibition]. Nahrung. 1977;21(4):311-7.

The limit of detection for aldicarb, baygon, benomyl, bux, carbaryl, CIPC, matacil, phenmedipham and promecarb lies in the picogram range; that for barban and methomyl, in the nanogram range.
1(0,0,0,1) Details
2386419 Goldman LR, Beller M, Jackson RJ: Aldicarb food poisonings in California, 1985-1988: toxicity estimates for humans. Arch Environ Health. 1990 May-Jun;45(3):141-7.

Estimated dosages ranged between 0.0023 [corrected] and 0.06 mg/kg body weight, and most were well below the 0.025 mg/kg Lowest Observed Effect Level (LOEL) for subclinical blood cholinesterase depression previously reported for humans.
1(0,0,0,1) Details
3822252 Bakry NM, Sherby SM, Eldefrawi AT, Eldefrawi ME: Oxadiazolidinones: irreversible inhibition of cholinesterases and effects on acetylcholine receptors. Neurotoxicology. 1986 Fall;7(3):1-10.

Aldicarb, a carbamate anticholinesterase, which protected Torpedo AChE against irreversible phosphorylation by DFP, also protected it against irreversible inhibition by DBOX and MPOX.
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8310452 Ahmed HM, Shoka AA: Toxic interactions between copper sulphate and some organic agrochemicals. Toxicol Lett. 1994 Jan;70(1):109-19.

Groups of rats were treated with graded doses of zineb or aldicarb solely or in association with copper sulphate for nine consecutive weeks.
Alanine aminotransferase (ALT) activity was significantly increased, while cholinesterase (ChE) activity was decreased in all treated groups.
1(0,0,0,1) Details
10227801 : Aldicarb as a cause of food poisoning--Louisiana, 1998. MMWR Morb Mortal Wkly Rep. 1999 Apr 9;48(13):269-71.

Cholinesterase-inhibiting pesticides (i.e., organic phosphates and carbamates), widely used in agriculture, can cause illness if they contaminate food or drinking water.
1(0,0,0,1) Details
3661796 Green MA, Heumann MA, Wehr HM, Foster LR, Williams LP Jr, Polder JA, Morgan CL, Wagner SL, Wanke LA, Witt JM: An outbreak of watermelon-borne pesticide toxicity. Am J Public Health. 1987 Nov;77(11):1431-4.

Residues of aldicarb, a cholinesterase inhibitor, were found in 10 of 16 tested melons which had been eaten by persons meeting the case definition.
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3304999 Risher JF, Mink FL, Stara JF: The toxicologic effects of the carbamate insecticide aldicarb in mammals: a review. Environ Health Perspect. 1987 Jun;72:267-81.

The primary mechanism of toxic action of aldicarb is cholinesterase inhibition.
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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 activity of cholinesterase is non-competitively inhibited in the presence of pesticides.
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18631301 Williams RL, Mihlan GJ, Tobia AJ: Modeling cholinesterase activity for human dietary risk assessment of carbamate insecticides. Risk Anal. 2008 Aug;28(4):1069-79. Epub 2008 Jul 9.

Repeated measurements were taken prior to exposure and at 1, 2, 4, 6, 8, and 21 hours after exposure to the carbamate aldicarb.
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10220078 Lifshitz M, Shahak E, Sofer S: Carbamate and organophosphate poisoning in young children. Pediatr Emerg Care. 1999 Apr;15(2):102-3.


The carbamate agents were identified as methomyl or aldicarb, and the organophosphate as parathion, fenthion, malathion, and diazinon.
0(0,0,0,0) Details
12209188 Yang R: NTP technical report on the toxicity studies of Pesticide/Fertilizer Mixtures Administered in Drinking Water to F344/N Rats and B6C3F1 Mice. Toxic Rep Ser. 1993 Aug;36:1-G3.


The California mixture was composed of aldicarb, atrazine, 1,2-dibromo-3-chloropropane, 1,2- dichloropropane, ethylene dibromide, simazine, and ammonium nitrate.
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2380482 Farage-Elawar M: Effects of in ovo injection of carbamates on chick embryo hatchability, esterase enzyme activity and locomotion of chicks. J Appl Toxicol. 1990 Jun;10(3):197-201.

Brain acetylcholinesterase (AChE) and liver cholinesterase (ChE) were inhibited significantly during incubation in embryos dosed on day 15 with both carbaryl and aldicarb.
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19165329 Wang J, Farr GW, Hall DH, Li F, Furtak K, Dreier L, Horwich AL: An ALS-linked mutant SOD1 produces a locomotor defect associated with aggregation and synaptic dysfunction when expressed in neurons of Caenorhabditis elegans. PLoS Genet. 2009 Jan;5(1):e1000350. Epub 2009 Jan 23.

Mutant animals were resistant to paralysis by the cholinesterase inhibitor aldicarb, while exhibiting normal sensitivity to the cholinergic agonist levamisole and normal muscle morphology.
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9772213 El-Alfy A, Schlenk D: Potential mechanisms of the enhancement of aldicarb toxicity to Japanese medaka, Oryzias latipes, at high salinity. Toxicol Appl Pharmacol. 1998 Sep;152(1):175-83.

In addition, salinity also seems to potentiate the anticholinesterase activity of aldicarb (the parent) through an unknown mechanism.
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1685431 Noel GR, Mayasich SO: Partial characterization of soluble esterase from Heterodera glycines and inhibition by aldicarb and phenamiphos. Comp Biochem Physiol C. 1991;99(3):537-40.

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15378568 Reuveny H, Cohen E: Evaluation of mechanisms of azinphos-methyl resistance in the codling moth Cydia pomonella (L.). Arch Insect Biochem Physiol. 2004 Oct;57(2):92-100.


Of the three carbamates examined, only carbaryl was inhibitory at the mM range while pirimicarb and aldicarb were inactive.
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2588705 Goedicke HJ, Hermes H, Wagner R: [Exposure to residues on plant surfaces following the use of plant pesticides in the greenhouse]. Z Gesamte Hyg. 1989 Sep;35(9):531-3.

Residues on plants, concentration in the air, dermal exposition, and inhibition of serum choline esterase activity are shown for methamidophos and aldicarb, respective reentry times being discussed.
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11404329 van Swinderen B, Metz LB, Shebester LD, Mendel JE, Sternberg PW, Crowder CM: Goalpha regulates volatile anesthetic action in Caenorhabditis elegans. Genetics. 2001 Jun;158(2):643-55.

Pharmacological assays using the cholinesterase inhibitor aldicarb suggest that VAs and GOA-1 similarly downregulate cholinergic neurotransmitter release in C. elegans.
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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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11936581 Tracqui A, Flesch F, Sauder P, Raul JS, Geraut A, Ludes B, Jaeger A: Repeated measurements of aldicarb in blood and urine in a case of nonfatal poisoning. Hum Exp Toxicol. 2001 Dec;20(12):657-60.

The patient's clinical picture closely followed blood aldicarb levels and serum pseudo-cholinesterase activities.
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11291736 Ragoucy-Sengler C, Tracqui A, Chavonnet A, Daijardin JB, Simonetti M, Kintz P, Pileire B: Aldicarb poisoning. Hum Exp Toxicol. 2000 Dec;19(12):657-62.

Serum cholinesterase activity was always lower than 30% of the normal range and aldicarb was identified by UV spectra and retention time after liquid chromatography separation.
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8214574 Hunt KA, Hooper MJ: Development and optimization of reactivation techniques for carbamate-inhibited brain and plasma cholinesterases in birds and mammals. Anal Biochem. 1993 Aug 1;212(2):335-43.

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17216925 Osman MY, Sharaf IA, Mohamed AS, Osman HM: Effect of the carbamate "aldicarb" on acetyl cholinesterase extracted from whole and different parts of rat brain (in vitro and in vivo studies). J Egypt Public Health Assoc. 2000;75(3-4):301-21.
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8747743 Moser VC: Comparisons of the acute effects of cholinesterase inhibitors using a neurobehavioral screening battery in rats. Neurotoxicol Teratol. 1995 Nov-Dec;17(6):617-25.

The acute effects of two carbamates (carbaryl, aldicarb) and five organophosphates (OP) (chlorpyrifos, diazinon, parathion, fenthion, and diisopropyl fluorophosphate, or DFP) were evaluated on the day of dosing at the time of peak effect, at 1 and 3 days, and 1 week after dosing (oral gavage, in corn oil).
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8548921 Rotenberg M, Almog S: Evaluation of the decarbamylation process of cholinesterase during assay of enzyme activity. Clin Chim Acta. 1995 Sep 15;240(2):107-16.

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11545234 Nelson LS, Perrone J, DeRoos F, Stork C, Hoffman RS: Aldicarb poisoning by an illicit rodenticide imported into the United States: Tres Pasitos. J Toxicol Clin Toxicol. 2001;39(5):447-52.

This study characterizes the ongoing epidemic of acute cholinesterase inhibitor poisoning due to an illicit rodenticide and identifies its etiology.
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