Protein Information

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

Compound Information

Name dimethoate
CAS

Reference List

PubMed Abstract RScore(About this table)
17997881 Wu QE, Yao XM, Ban TT, Jiang N, Shao CF, Chang XL, Zhou ZJ: [Effects of 90-day oral dimethoate exposure on glutamatergic system and neurobehavioral performance in rats]. Zhonghua Lao Dong Wei Sheng Zhi Ye Bing Za Zhi. 2007 Sep;25(9):513-7.

AChE activity was significantly reduced 42% approximately 78% by all three doses of dimethoate (P < 0.05).
82(1,1,1,2) 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
719292 Buckley GA, Godden DH, Parrish SK: Motor output to flight muscles and inhibition of acetylcholinesterase after injection of dimethoate into locusts [proceedings] Br J Pharmacol. 1978 Nov;64(3):446P-447P.
81(1,1,1,1) Details
17374424 Augustyniak M, Migula P, Mesjasz-Przybylowicz J, Tarnawska M, Nakonieczny M, Babczynska A, Przybylowicz W, Augustyniak MG: Short-term effects of dimethoate on metabolic responses in Chrysolina pardalina (Chrysomelidae) feeding on Berkheya coddii (Asteraceae), a hyper-accumulator of nickel. Environ Pollut. 2007 Nov;150(2):218-24. Epub 2007 Mar 19.

Data recorded included the activity of acetylcholinesterase (AChE), the concentration of glutathione (GSH), and the activity of selected enzymes connected with GSH metabolism.
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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
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.
2(0,0,0,2) Details
11985885 Yang D, Lu X, Zhang W, He F: Biochemical changes in primary culture of skeletal muscle cells following dimethoate exposure. Toxicology. 2002 May 24;174(2):79-85.

In order to investigate the cellular mechanism of muscular weakness in the Intermediate Myasthenia Syndrome (IMS) following acute organophosphate poisoning, we studied the cytotoxicity of dimethoate and its effects on the activity of acetylcholine esterase (AChE), Na+-K+-ATPase, succinate dehydrogenase (SDH), and Ca2+-ATPase in primary cultured skeletal muscle cells.
62(0,2,2,2) Details
18384757 Eyer P, Radtke M, Worek F: Reactions of isodimethoate with human red cell acetylcholinesterase. . Biochem Pharmacol. 2008 May 15;75(10):2045-53. Epub 2008 Feb 26.

Isodimethoate shows an inhibition rate constant towards human red blood cell acetylcholinesterase (AChE) of 2.3x10 (3) M (-1) min (-1) (pH 7.4, 37 degrees C), indicating a somewhat higher potency than found with omethoate, the CYP450-mediated active metabolite of pure dimethoate.
46(0,1,3,6) Details
7481747 Johnston G: The study of interactive effects of pollutants: a biomarker approach. Sci Total Environ. 1995 Oct 27;171(1-3):205-12.

Biochemical biomarkers, such as inhibition of serum butyryl cholinesterase (BuChE) and brain acetyl cholinesterase (AChE), have been useful in studies of interactive effects of pesticides in birds.
Birds pretreated with prochloraz showed a trend towards greater inhibition of serum BuChE activity at most time points following dosing with the OPs dimethoate and chlorpyriphos.
2(0,0,0,2) Details
9074804 Mahajna M, Quistad GB, Casida JE: Acephate insecticide toxicity: safety conferred by inhibition of the bioactivating carboxyamidase by the metabolite methamidophos. Chem Res Toxicol. 1997 Jan;10(1):64-9.

Acephate is an important systemic organophosphorus insecticide with toxicity attributed to bioactivation on metabolic conversion to methamidophos (or an oxidized metabolite thereof) which acts as an acetylcholinesterase (AChE) inhibitor.
Methamidophos pretreatment in rats also markedly alters the metabolism of dimethoate (another systemic insecticide) from principally carboxyamide hydrolysis to mainly other pathways.
2(0,0,0,2) Details
15779760 Engenheiro EL, Hankard PK, Sousa JP, Lemos MF, Weeks JM, Soares AM: Influence of dimethoate on acetylcholinesterase activity and locomotor function in terrestrial isopods. Environ Toxicol Chem. 2005 Mar;24(3):603-9.
42(0,1,2,7) Details
20169407 Mdegela RH, Mosha RD, Sandvik M, Skaare JU: Assessment of acetylcholinesterase activity in Clarias gariepinus as a biomarker of organophosphate and carbamate exposure. Ecotoxicology. 2010 Feb 19.

Concentrations of pesticides that inhibited 50% (IC (50)) of AChE activities in brain homogenates following in vitro exposures were 0.003, 0.03, 0.15, 190, 0.2, 0.003 and 0.002 muM for carbaryl, chlorfenvinphos, diazinon, dimethoate, fenitrothion, pirimiphosmethyl and profenofos, respectively.
40(0,1,1,10) Details
2973491 Shaker N, Hassan GA, el-Nouty FD, Abo-Elezz Z, Abd-Allah GA: In vivo chronic effect of dimethoate and deltamethrin on rabbits. J Environ Sci Health B. 1988 Aug;23(4):387-99.

AChE activity was increased (P less than 0.01) after 1 month of treatment with the two doses of dimethoate and deltamethrin; thereafter, AChE activity showed 40% inhibition of the control level.
37(0,1,2,2) Details
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.

2(0,0,0,2) Details
16704047 Andersen TH, Tjornhoj R, Wollenberger L, Slothuus T, Baun A: Acute and chronic effects of pulse exposure of Daphnia magna to dimethoate and pirimicarb. Environ Toxicol Chem. 2006 May;25(5):1187-95.

The most important new findings in the present study are that short-term (<4 h) pulse exposure of neonates to acetylcholinesterase-inhibiting pesticides caused reproductive damage in D. magna and that repeated-pulse exposure significantly increased mortality in animals that apparently had recovered after a single-pulse exposure.
1(0,0,0,1) Details
6738494 Fetcher A: Suspected dimethoate toxicity in cattle. Mod Vet Pract. 1984 Apr;65(4):283-5.

Whole blood acetylcholinesterase activity was depressed in 3 animals.
1(0,0,0,1) Details
16708891 Roy R, Chaudhuri AN: Differential acetylcholinesterase activity in rat cerebrum, cerebellum and hypothalamus. Indian J Exp Biol. 2006 May;44(5):381-6.

Purified and lyophilized AChE from different (NH4) 2SO4 precipitated fractions of three brain parts were utilized for in vitro enzyme kinetics using Dimethoate (Dmt) as inhibitor.
35(0,1,1,5) Details
18625401 Kakani EG, Ioannides IM, Margaritopoulos JT, Seraphides NA, Skouras PJ, Tsitsipis JA, Mathiopoulos KD: A small deletion in the olive fly acetylcholinesterase gene associated with high levels of organophosphate resistance. Insect Biochem Mol Biol. 2008 Aug;38(8):781-7. Epub 2008 May 22.

In addition, remaining activity of acetylcholinesterase enzyme (AChE) after dimethoate inhibition was higher in genotypes carrying the mutation.
34(0,1,1,4) Details
985225 Stone BF, Wilson JT, Youlton NJ: Linkage and dominance characteristics of genes for resistance to organophosphorus acaricides and allelic inheritance of decreased brain cholinesterase activity in three strains of the cattle tick, Boophilus microplus. Aust J Biol Sci. 1976 Jul;29(3):251-63.

This evidence was strongly suggestive of a series of closely linked genes or alleles controlling dimethoate resistance and a series of alleles controlling decreased brain AChE activity in strains B, M and R.
32(0,1,1,2) Details
12185494 Pavlic M, Haidekker A, Grubwieser P, Rabl W: Fatal intoxication with omethoate. Int J Legal Med. 2002 Aug;116(4):238-41. Epub 2002 Apr 17.


The amount of the active AChE in peripheral blood serum was reduced to less than 0.2% of the normal level.
1(0,0,0,1) Details
1063663 Devonshire AL, Sawicki RM: The importance of the decreased susceptibility of acetylcholinesterase in the resistance of houseflies to organophosphorus insecticides. Environ Qual Saf Suppl. 1975;3:441-6.

1(0,0,0,1) Details
8698421 Srivastava MK, Raizada RB: Development effect of technical dimethoate in rats: maternal and fetal toxicity evaluation. Indian J Exp Biol. 1996 Apr;34(4):329-33.

Reduced acetylcholinesterase activity in fetal brain and placenta at higher dose levels indicated possible transmigration of dimethoate from dams to fetuses.
31(0,1,1,1) Details
16906295 Campagna AF, Eler MN, Espindola EL, Senhorini JA, do Rego RF, Silva LO: Dimethoate 40% organosphosphorous pesticide toxicity in Prochilodus lineatus (Prochilodontidae, Characiformes) eggs and larvae. Braz J Biol. 2006 May;66(2B):633-40.

It was chosen for testing different concentrations of 40% dimethoate, an organophosphate insecticide and acetylcholinesterase enzyme (AChE) inhibitor used widely in Brazil.
31(0,1,1,1) Details
16833148 Long SM, Dawson A, Shore RF: A comparison of the effects of single and repeated exposure to an organophosphate insecticide on acetylcholinesterase activity in mammals. Environ Toxicol Chem. 2006 Jul;25(7):1857-63.

We compared the effects of single or repeated (hourly and daily) exposure to dimethoate on acetylcholinesterase (AChE) activity in laboratory mice to assess the suitability of standard laboratory tests for assessing risk.
20(0,0,3,5) Details
2588727 Deike S, Wosnitzka H: [Behavior of serum cholinesterase and acetylcholinesterase activity in acute dimethoate poisoning]. Z Gesamte Inn Med. 1989 Sep 15;44(18):548-9.
13(0,0,2,3) Details
12101633 Coeurdassier M, Gomot-De Vaufleury A, Saint-Denis M, Ribera D, Narbonne JF, Badot PM: Effects of dimethoate on snail B-esterase and growth as a function of dose, time and exposure route in a laboratory bioassay. Biomarkers. 2002 Mar-Apr;7(2):138-50.

The present results show that AChE activity could be used to give early warning of toxic effects of dimethoate in terrestrial gastropods.
12(0,0,1,7) Details
16718740 Kristensen M, Huang J, Qiao CL, Jespersen JB: Variation of Musca domestica L. acetylcholinesterase in Danish housefly populations. Pest Manag Sci. 2006 Aug;62(8):738-45.

A comparison was made of toxicological data and AChE activity gathered from 21 field populations and nine laboratory strains of houseflies, Musca domestica L., to elucidate the best way of generating data to provide advice for management strategies and gathering information for resistance risk assessment on the organophosphates azamethiphos and dimethoate and the carbamate methomyl, which have been the primary insecticides used against adult houseflies in Denmark.
10(0,0,1,5) Details
18569613 Rajini PS, Melstrom P, Williams PL: A comparative study on the relationship between various toxicological endpoints in Caenorhabditis elegans exposed to organophosphorus insecticides. J Toxicol Environ Health A. 2008;71(15):1043-50.

The toxicity of 10 organophophorus (OP) insecticides-acephate, dimethoate, dichlorvos, dicrotophos, monocrotophos, methamidophos, phosphamidon, omethoate, phosdrin, and trichlorfon-was evaluated in Caenorhabditis elegans using lethality, movement, and acetylcholinesterase (AChE) activity as the endpoints after a 4-hr- exposure period.
9(0,0,1,4) Details
19917271 Worek F, Aurbek N, Herkert NM, John H, Eddleston M, Eyer P, Thiermann H: Evaluation of medical countermeasures against organophosphorus compounds: The value of experimental data and computer simulations. Chem Biol Interact. 2009 Nov 13.

In the present study, in vitro enzyme-kinetic and pharmacokinetic data from a minipig model of dimethoate poisoning and oxime treatment were used to calculate dynamic changes of AChE activities.
9(0,0,1,4) Details
11521821 Coeurdassier M, Saint-Denis M, Gomot-de Vaufleury A, Ribera D, Badot PM: The garden snail (Helix aspersa) as a bioindicator of organophosphorus exposure: effects of dimethoate on survival, growth, and acetylcholinesterase activity. Environ Toxicol Chem. 2001 Sep;20(9):1951-7.
8(0,0,1,3) Details
19069555 Nazarian A: Utilization of dimethoate by wild type Pseudomonas putida from polluted sites in Iran. Pak J Biol Sci. 2007 Feb 15;10(4):664-7.

Anti-acetyl choline esterase (AChE) Activity was proportionally displayed of dimethoate level (0.2-2 g L (-1)).
7(0,0,1,2) Details
19778190 Thiermann H, Worek F, Eyer P, Eyer F, Felgenhauer N, Zilker T: Obidoxime in acute organophosphate poisoning: 2 - PK/PD relationships. Clin Toxicol. 2009 Sep;47(8):807-13.


In this article we report effects on neuromuscular function, oxime and atropine concentration, and relate them to acetylcholinesterase (AChE) activity.
6(0,0,0,6) Details
19908228 Carletto J, Martin T, Vanlerberghe-Masutti F, Brevault T: Insecticide resistance traits differ among and within host races in Aphis gossypii. Pest Manag Sci. 2010 Mar;66(3):301-7.

Conversely, all clones were resistant to dimethoate (organophosphate) (RF = 4.1-38.1) and carried mutation S431F in the acetylcholinesterase gene.
6(0,0,1,1) Details
1586201 al-Jaghbir MT, Salhab AS, Hamarsheh FA: Dermal and inhalation exposure to dimethoate. . Arch Environ Contam Toxicol. 1992 May;22(4):358-61.

Dermal and respiratory exposure and plasma acetylcholinesterase (ChE) activity were monitored on six workers spraying tomato crops under plastic houses with dimethoate [O,O-dimethyl S-(N-methylcarbamoylmethyl) phosphorodithoate].
6(0,0,1,1) Details
8975827 Dell'Omo G, Shore RF: Behavioral effects of acute sublethal exposure to dimethoate on wood mice, Apodemus sylvaticus: II--Field studies on radio-tagged mice in a cereal ecosystem. Arch Environ Contam Toxicol. 1996 Nov;31(4):538-42.

Male mice were radio-tagged at night and followed during 2-3-d periods, before and after an intraperitoneal injection of 50 mg/kg dimethoate which previous laboratory studies had demonstrated causes a maximum depression in brain acetylcholinesterase (AChE) activity of 75% relative to non-exposed mice.
6(0,0,1,1) Details
12144698 Vontas JG, Hejazi MJ, Hawkes NJ, Cosmidis N, Loukas M, Janes RW, Hemingway J: Resistance-associated point mutations of organophosphate insensitive acetylcholinesterase, in the olive fruit fly Bactrocera oleae. Insect Mol Biol. 2002 Aug;11(4):329-36.

5(0,0,0,5) Details
19883634 Eyer P, Worek F, Thiermann H, Eddleston M: Paradox findings may challenge orthodox reasoning in acute organophosphate poisoning. Chem Biol Interact. 2009 Oct 31.

Dimethylphosphorylated AChE is in general less amenable to oxime therapy, which largely fails in some cases of dimethoate poisoning where aging was much faster than expected from a dimethylphosphorylated enzyme.
It is generally accepted that inhibition of acetylcholinesterase (AChE) is the most important acute toxic action of organophosphorus compounds, leading to accumulation of acetylcholine followed by a dysfunction of cholinergic signaling.
5(0,0,0,5) Details
16701032 Xie F, Zhou ZJ, Wu TJ, Wu QE, Shao CF, Ban TT: [Effect of dimethoate on the expression of heat shock protein 70 in peripheral blood lymphocytes of human beings]. Zhonghua Lao Dong Wei Sheng Zhi Ye Bing Za Zhi. 2006 Apr;24(4):214-7.

The activity of whole blood acetylcholinesterase (AChE) was examined at the same time.
4(0,0,0,4) Details
16914184 Babczynska A, Wilczek G, Migula P: Effects of dimethoate on spiders from metal pollution gradient. Sci Total Environ. 2006 Nov 1;370(2-3):352-9. Epub 2006 Aug 17.

Then the activities of detoxifying (carboxylesterase: CarE, glutathione S-transferase: GST), antioxidative (selene-dependent and selene-independent glutathione peroxidases: GPOX and GSTPx) enzymes as well as acetylcholinesterase as a biomarker of exposure to OP pesticides were measured.
4(0,0,0,4) Details
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.
4(0,0,0,4) Details
19778163 Eyer F, Worek F, Eyer P, Felgenhauer N, Haberkorn M, Zilker T, Thiermann H: Obidoxime in acute organophosphate poisoning: 1 - clinical effectiveness. Clin Toxicol. 2009 Sep;47(8):798-806.

In this article we report clinical findings and activity of cholinesterase in plasma and acetylcholinesterase (AChE) in red blood cells.
METHODS: We studied 34 atropinized patients with severe parathion, oxydemeton methyl, and dimethoate self-poisoning who were treated with obidoxime in a standard protocol.
4(0,0,0,4) Details
18070496 Wan WG, Zheng SC, Zou HJ, Ma SD, Tao GZ, Xu ZF, Zhang B, Chen JJ, Fang LY, Zhu ZJ: [Different therapeutic efficacy of parlidoxime chloride PAM-Cl on AChE against acute toxicity of methamidophos, dichlorovs and omethoate]. Zhonghua Lao Dong Wei Sheng Zhi Ye Bing Za Zhi. 2007 Oct;25(10):586-9.

METHODS: 101 patients with AOPP in 7 hospitals were divided into three groups: Group A, 59 patients with acute methamidophos poisoning, Group B, 32 patients with acute DDV/dipterex (DEP) poisoning, Group C, 10 patients with acute omethoate/dimethoate poisoning.
3(0,0,0,3) 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
10207609 Worek F, Diepold C, Eyer P: Dimethylphosphoryl-inhibited human cholinesterases: inhibition, reactivation, and aging kinetics. Arch Toxicol. 1999 Feb;73(1):7-14.

Human poisoning by organophosphates bearing two methoxy groups, e.g. by malathion, paraoxon-methyl, dimethoate and oxydemeton-methyl, is generally considered to be rather resistant to oxime therapy.
The efficacy of obidoxime in reactivating dimethylphosphoryl-AChE was 40, 9 and 3 times higher than of HI 6, pralidoxime and HLo 7, respectively.
3(0,0,0,3) Details
16112538 Rios JC, Repetto G, Galleguillos I, Jos A, Peso AD, Repetto M: High concentrations of pralidoxime are needed for the adequate reactivation of human erythrocyte acetylcholinesterase inhibited by dimethoate in vitro. Toxicol In Vitro. 2005 Oct;19(7):893-7. Epub 2005 Aug 19.
163(2,2,2,3) Details
16573274 Barski D, Zasadowski A: Residues of dimethoate in the liver and AchE activity in blood of rats after exposure to dimethoate, and dimethoate and pyrantel embonate. Pol J Vet Sci. 2006;9(1):43-9.

Dimethoate in both applied doses significantly reduced AChE activity in blood.
88(1,1,2,3) Details
15033006 Sun YG, Zhou ZJ, Zhang XM, Gu XA, Jin TY: [Muscarine receptor gene expression in brain and peripheral blood lymphocytes of rats pretreated with dimethoate for 28 days]. Zhonghua Lao Dong Wei Sheng Zhi Ye Bing Za Zhi. 2004 Feb;22(1):7-10.

The activity of whole blood acetylcholinesterase (AChE) was examined.
3(0,0,0,3) Details
19428953 Aurbek N, Thiermann H, Eyer F, Eyer P, Worek F: Suitability of human butyrylcholinesterase as therapeutic marker and pseudo catalytic scavenger in organophosphate poisoning: a kinetic analysis. Toxicology. 2009 May 17;259(3):133-9. Epub 2009 Mar 6.

The toxic symptomatology is caused by inhibition of acetylcholinesterase (AChE).
As oxime efficacy is limited with certain OPs (e.g. dimethoate, tabun, soman) alternative therapeutic approaches, e.g. the application of scavengers (BChE) which may sequester OPs before they reach their physiological target, are under investigation.
3(0,0,0,3) Details
985226 Stone BF, Nolan J, Schuntner CA: Biochemical genetics of resistance to organophosphorus acaricides in three strains of the cattle tick, Boophilus microplus. Aust J Biol Sci. 1976 Jul;29(3):265-79.

Dimethoxon inhibition of AChE in brains, their homogenates and larval homogenates of B, M and R types showed that decreased AChE sensitivity was a major mechanism of resistance to dimethoate strongly expressed in B x S and M x S hybrids.
87(1,1,1,7) Details
17590326 Du D, Huang X, Cai J, Zhang A: Comparison of pesticide sensitivity by electrochemical test based on acetylcholinesterase biosensor. Biosens Bioelectron. 2007 Sep 30;23(2):285-9. Epub 2007 May 18.

Four pesticides of carbaryl, malathion, dimethoate and monocrotophos were selected to discuss their inhibition efficiencies to AChE.
85(1,1,1,5) Details
6871453 Braginskaia FI, Sultanova GG, Zorina OM: [Effect of chlorine-containing pesticides on the hemolytic stability and acetylcholinesterase activity of erythrocytes]. Biull Eksp Biol Med. 1983 Jul;96(7):36-8.

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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.
83(1,1,1,3) Details
16496292 Farag AT, Karkour TA, El Okazy A: Developmental toxicity of orally administered technical dimethoate in rats. Birth Defects Res B Dev Reprod Toxicol. 2006 Feb;77(1):40-6.

CONCLUSIONS: On the basis of the present results dimethoate can produce clinical signs of toxicity and significant inhibition of the maternal and fetal AChE activities in dose groups of 15 and 28 mg/kg/day and showed fetotoxicity without teratogenic effects at 28 mg/kg/day.
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16112789 Sharma Y, Bashir S, Irshad M, Nag TC, Dogra TD: Dimethoate-induced effects on antioxidant status of liver and brain of rats following subchronic exposure. Toxicology. 2005 Nov 15;215(3):173-81. Epub 2005 Aug 19.

This study concludes that oxidative stress due to dimethoate may be ascribed to induction of Cytochrome P450, inhibition of AChE and disturbance in activities of GSH and GST enzymes causing lipid peroxidation and histological and electron microscopic changes in liver and brain.
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7316761 Lotti M, Ferrara SD, Caroldi S, Sinigaglia F: Enzyme studies with human and hen autopsy tissue suggest omethoate does not cause delayed neuropathy in man. Arch Toxicol. 1981 Nov;48(4):265-70.


Levels of acetylcholinesterase and neurotoxic esterase were measured in brain autopsy material.
2(0,0,0,2) Details
2841086 Besser R, Dillmann U, Gutmann L, Hopf HC: [The repetitive muscular action potential in neuromuscular transmission disorders due to acetylcholinesterase inhibition]. EEG EMG Z Elektroenzephalogr Elektromyogr Verwandte Geb. 1988 Jun;19(2):85-91.

1(0,0,0,1) Details
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.
We also discuss case reports where neuropathies were not convincingly attributed to fenthion, malathion, omethoate/dimethoate, parathion and merphos.
1(0,0,0,1) Details
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
17234381 Farag AT, El-Aswad AF, Shaaban NA: Assessment of reproductive toxicity of orally administered technical dimethoate in male mice. Reprod Toxicol. 2007 Feb;23(2):232-8. Epub 2006 Dec 22.

Brain and skeletal muscle acetylcholinesterase activities were inhibited in both the middle and high dose groups.
1(0,0,0,1) Details
9619645 Singh G, Mahajan R, Whig J: The importance of electrodiagnostic studies in acute organophosphate poisoning. J Neurol Sci. 1998 May 7;157(2):191-200.


Electrodiagnostic studies revealed single stimulus induced repetitive responses and decrement-increment responses at 30 and 50 Hz repetitive nerve stimulation, findings that are indicative of a depolarization block due to inactivation of acetylcholinesterase at the motor end-plate.
1(0,0,0,1) Details
224645 Sterri SH, Rognerud B, Fiskum SE, Lyngaas S: Effect of toxogonin and P2S on the toxicity of carbamates and organophosphorus compounds. Acta Pharmacol Toxicol. 1979 Jul;45(1):9-15.

Toxogonin (80 mg/kg intraperitoneally) given 15 min. prior to the administration of organophosphorus insecticides dimethoate, malathion, parathion and azinphos-methyl, organophosphorus warfare agents soman and tabun, or carbamates physostigmine, pyridostigmine and aldicarb, reduced the toxicity in mice of these agents by increasing their LD50 dose 1.5-3 fold.
The acetylcholinesterase activity in erythrocytes, cerebrum and diaphragm of surviving mice 20 hours after organophosphate intoxication was similar both in toxogonin and P2S treated animals and untreated animals.
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9174953 Tran-Minh C: Biosensors in flow-injection systems for biomedical analysis, process and environmental monitoring. J Mol Recognit. 1996 Sep-Dec;9(5-6):658-63.


Acetylcholinesterase sensors have been used in batch systems for the determination of pesticides, but they require large amounts of substrate.
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11681666 Maklakov A, Ishaaya I, Freidberg A, Yawetz A, Horowitz AR, Yarom I: Toxicological studies of organophosphate and pyrethroid insecticides for controlling the fruit fly Dacus ciliatus (Diptera: Tephritidae). J Econ Entomol. 2001 Oct;94(5):1059-66.


This was supported by the insignificant decrease of head acetylcholinesterase activity.
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15590108 Sharma Y, Bashir S, Irshad M, Gupta SD, Dogra TD: Effects of acute dimethoate administration on antioxidant status of liver and brain of experimental rats. Toxicology. 2005 Jan 5;206(1):49-57.

Erythrocyte acetylcholinesterase was inhibited at all doses used.
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9143451 Mohapatra PK, Schubert H, Schiewer U: Effect of dimethoate on photosynthesis and pigment fluorescence of Synechocystis sp. Ecotoxicol Environ Saf. 1997 Apr;36(3):231-7.

The organophosphorus (OP) insecticides are powerful inhibitors of esterases, and their toxic actions are commonly explained in terms of acetylcholinesterase (EC 3.1.1.7) inhibition but their phytotoxic effects remain unexplained.
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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.
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20106727 John H, Eddleston M, Clutton RE, Worek F, Thiermann H: Simultaneous quantification of the organophosphorus pesticides dimethoate and omethoate in porcine plasma and urine by LC-ESI-MS/MS and flow-injection-ESI-MS/MS. J Chromatogr B Analyt Technol Biomed Life Sci. 2010 Jan 14.

It also exhibits toxic activity towards mammalian organism provoked by catalytic desulfuration in the liver producing its oxon-derivative omethoate thus inhibiting acetylcholinesterase, initiating cholinergic crisis and ultimately leading to death by respiratory paralysis and cardiovascular collapse.
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954759 Okonek S, Boelcke G, Hollmann H: Therapeutic properties.of haemodialysis and blood exchange transfusion in organophosphate poisoning. Eur J Intensive Care Med. 1976;2(1):13-8.

Human blood was contaminated with nitrostigmine, dimethoate and demeton-S-methyl sulfoxide.
Acetylcholinesterase activity increased only briefly in the period of blood exchange transfusion and decreased gradually afterwards.
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2539961 Besser R, Hopf HC, Gutmann L, Dillmann U: [The decrement-increment phenomenon in disorders of neuromuscular transmission by inhibition of acetylcholinesterase]. EEG EMG Z Elektroenzephalogr Elektromyogr Verwandte Geb. 1989 Mar;20(1):28-33.

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16257584 Augustyniak M, Babczynska A, Migula P, Wilczek G, Laszczyca P, Kafel A, Augustyniak M: Joint effects of dimethoate and heavy metals on metabolic responses in a grasshopper (Chorthippus brunneus) from a heavy metals pollution gradient. Comp Biochem Physiol C Toxicol Pharmacol. 2005 Aug;141(4):412-9. Epub 2005 Oct 28.

Inhibition of acetylcholinesterase (AChE) reaches nearly 50% of the value stated in untreated insects, without significant site-dependent differences.
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8658539 Marinovich M, Ghilardi F, Galli CL: Effect of pesticide mixtures on in vitro nervous cells: comparison with single pesticides. Toxicology. 1996 Apr 30;108(3):201-6.


The toxicity of dimethoate, azinphos-methyl, diazinon, pirimiphos methyl, organophosphorus insecticides, and benomyl (a benzimidazole fungicide) singly and in mixture was studied in a human neuroblastoma cell line, SH-SY5Y.
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8473001 Krieger RI, Thongsinthusak T: Metabolism and excretion of dimethoate following ingestion of overtolerance peas and a bolus dose. Food Chem Toxicol. 1993 Mar;31(3):177-82.

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11834209 John S, Kale M, Rathore N, Bhatnagar D: Protective effect of vitamin E in dimethoate and malathion induced oxidative stress in rat erythrocytes. J Nutr Biochem. 2001 Sep;12(9):500-504.

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11802337 Vos EM, Hens JJ, Lau HS, Boon ES, Bartelink AK: [Poisoning with organophosphate compounds] . Ned Tijdschr Geneeskd. 2002 Jan 5;146(1):34-7.

This case is characteristic for acute intoxications with irreversible acetylcholinesterase inhibitors, such as organophosphate compounds.
A 50-year-old man swallowed 200 ml of an insecticide containing the organophosphates dimethoate and phenitrotion in an attempted suicide.
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