Protein Information

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

Compound Information

Name demeton
CAS

Reference List

PubMed Abstract RScore(About this table)
18767757 Ghadamyari M, Talebi K, Mizuno H, Kono Y: Oxydemeton-methyl resistance, mechanisms, and associated fitness cost in green peach aphids (Hemiptera: Aphididae). J Econ Entomol. 2008 Aug;101(4):1432-8.


Susceptibility to oxydemeton-methyl and imidacloprid, and the inhibitory effects of oxydemeton-methyl and some organophosphate compounds on acetylcholinesterase (AChE) and carboxylesterase activity were studied in two populations (Karaj and Rasht) of green peach aphids, Myzus persicae (Sulzer).
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10421489 Richards P, Johnson M, Ray D, Walker C: Novel protein targets for organophosphorus compounds. Chem Biol Interact. 1999 May 14;119-120:503-11.

Rates of reaction of these labelling sites with a range of OP compounds were compared to that of acetylcholinesterase.
Neither labelling band reacted with chlorfenvinphos or demeton-s-methyl at significant rates.
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7726573 Lai K, Stolowich NJ, Wild JR: Characterization of P-S bond hydrolysis in organophosphorothioate pesticides by organophosphorus hydrolase. Arch Biochem Biophys. 1995 Apr 1;318(1):59-64.

The extensive use of organophosphorothioate insecticides in agriculture has resulted in the risk of environmental contamination with a variety of broadly based neurotoxins that inhibit the acetylcholinesterases of many different animal species.
Phosphorothiolate esters, such as demeton-S, provided noncompetitive inhibition for paraoxon (a P-O triester) hydrolysis, suggesting that the binding of these two different classes of substrates was not identical.
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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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15522601 Anitha K, Mohan SV, Reddy SJ: Development of acetylcholinesterase silica sol-gel immobilized biosensor--an application towards oxydemeton methyl detection. Biosens Bioelectron. 2004 Nov 1;20(4):848-56.

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9292288 Thiermann H, Mast U, Klimmek R, Eyer P, Hibler A, Pfab R, Felgenhauer N, Zilker T: Cholinesterase status, pharmacokinetics and laboratory findings during obidoxime therapy in organophosphate poisoned patients. Hum Exp Toxicol. 1997 Aug;16(8):473-80.


By virtue of in vitro findings and theoretical considerations we concluded in the preceding paper that oximes should preferably be administered by continuous infusion following an initial bolus dose for as long as reactivation of inhibited acetylcholinesterase (AChE) can be expected.
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20132373 Schofield DA, Dinovo AA: Generation of a mutagenized organophosphorus hydrolase for the biodegradation of the organophosphate pesticides malathion and demeton-S. J Appl Microbiol. 2010 Jan 11.

Activity was associated with organophosphate detoxification as the hydrolysed substrate lost the ability to inhibit acetylcholinesterase.
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11118318 Gopal S, Rastogi V, Ashman W, Mulbry W: Mutagenesis of organophosphorus hydrolase to enhance hydrolysis of the nerve agent VX. Biochem Biophys Res Commun. 2000 Dec 20;279(2):516-9.

Based on the crystal structure of OPH and the similarities it shares with acetylcholinesterase, eight OPH mutants were constructed with the goal of increasing OPH activity toward VX.
The activities of crude extracts from these mutants were measured using VX, demeton-S methyl, diisopropylfluoro-phosphate, ethyl parathion, paraoxon, and EPN as substrates.
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17590134 Perayre Badia M, Leiva Badosa E, Pasto Cardona L, Jodar Massanes R: [Intermediate syndrome after organophosphate poisoning despite continuous infusion of pralidoxime]. An Med Interna. 2007 Mar;24(3):129-31.


Acute organophosphate poisoning leads to a cholinergic crisis secondary to an acetylcholine rise, developed by an acetylcholinesterase inhibition.
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15629114 Fischer S, Arad A, Margalit R: Lipsome-formulated enzymes for organophosphate scavenging: butyrylcholinesterase and Demeton-S. Arch Biochem Biophys. 2005 Feb 1;434(1):108-15.

Monolayers of PC-12 cells were selected for feasibility testing based on: high affinity binding of the bioadhesive liposomes-DeltaG0 release upon binding ranged from -9 to -12 kcal/mol ligand; ability to mimic an organophosphate attack upon intact cells and measuring its impact on intracellular acetylcholinesterase.
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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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2307312 Clemens GR, Hartnagel RE, Bare JJ, Thyssen JH: Teratological, neurochemical, and postnatal neurobehavioral assessment of METASYSTOX-R, an organophosphate pesticide in the rat. Fundam Appl Toxicol. 1990 Jan;14(1):131-43.


Furthermore, the study was designed to determine if maternally toxic doses of MSR altered fetal brain acetylcholinesterase (AChE), compromised neonatal survival, growth, and development, or affected neurobehavioral development.
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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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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.

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7237776 Lewis PJ, Lowing RK, Gompertz D: Automated discrete kinetic method for erythrocyte acetylcholinesterase and plasma cholinesterase. Clin Chem. 1981 Jun;27(6):926-9.

To emphasize the need for measuring both erythrocyte acetylcholinesterase and plasma cholinesterase activity in workers exposed to organophosphate pesticides, we present a study of serial activities of both enzymes in a person accidentally exposed to demeton-S-methyl.
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16766477 Cho TM, Wild JR, Donnelly KC, Tiffany-Castiglioni E: Degradation of organophosphorus neurotoxicity in SY5Y neuroblastoma cells by organophosphorus hydrolase (OPH). J Toxicol Environ Health A. 2006 Aug;69(15):1413-29.

Anti-AChE activities of mipafox, methyl parathion, and demeton-S were partially ameliorated, depending on OP concentration.
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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.
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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.
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10414801 Thiermann H, Szinicz L, Eyer F, Worek F, Eyer P, Felgenhauer N, Zilker T: Modern strategies in therapy of organophosphate poisoning. Toxicol Lett. 1999 Jun 30;107(1-3):233-9.


At paraoxon concentrations > 0.1 microM obidoxime only partially reactivated acetylcholinesterase (AChE) of erythrocytes in vivo although reactivation could be assessed in vitro, which roughly fitted theoretical calculations.
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10207609 Worek F, Diepold C, Eyer P: Dimethylphosphoryl-inhibited human cholinesterases: inhibition, reactivation, and aging kinetics. Arch Toxicol. 1999 Feb;73(1):7-14.


The efficacy of obidoxime in reactivating dimethylphosphoryl-AChE was 40, 9 and 3 times higher than of HI 6, pralidoxime and HLo 7, respectively.
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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.
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