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1,1-dimethyl-4-acetylthiomethylpiperidinium + H2O
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i.e. MATP+, paper spray mass spectrometry is used to monitor the activity of acetylcholinesterase, both in-solution and on modified hydrophobic paper surface. Hydrophobic paper surfaces are prepared using vaporized trichloro(3,3,3-trifluoropropyl)silane. In both approaches, mixtures of diluted human whole blood with and without inhibitor ethyl ((2-[bis(propan-2-yl)amino]ethyl)sulfanyl)(methyl)phosphonate (VX) are mixed with a non-endogenous AChE specific substrate, 1,1-dimethyl-4-acetylthiomethylpiperidinium (MATP+). Formation of the cleaved MATP+ product is monitored over time and compared to MATP+ to determine relative AChE activity. This on-substrate assay is effective at determining AChE activity and identifying the toxicant, while determination of AChE activity in-solution proceeds at a slower rate. Method evaluation, overview
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1-naphthyl acetate + H2O
1-naphthol + acetate
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a chromogenic substrate for detection of erythrocyte acetylcholinesterase activity
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2,6-dichloro-3'-methylindophenylacetate + H2O
2,6-dichloro-3'-methylindophenol + acetate
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weak substrate
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2,6-dichlorophenolindophenol acetate + H2O
2,6-dichlorophenolindophenol + acetate
2,6-dichlorophenolindophenol acetate computational molecular docking study using the enzyme's crystal structure, PDB ID 4YE7
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2,6-dichlorophenolindophenylacetate + H2O
2,6-dichlorophenolindophenol + acetate
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2-methoxyacetylthiocholine + H2O
thiocholine + 2-methoxyacetate
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recombinant enzyme shows about 12% activity compared to acetylthiocholine
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?
3',5'-dichloro-2'-methylindophenylacetate + H2O
3',5'-dichloro-2'-methylindophenol + acetate
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weak substrate
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?
3',5'-dichlorophenolindophenylacetate + H2O
3',5'-dichlorophenolindophenol + acetate
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weak substrate
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?
3-(acetamido)-N,N,N-trimethylanilinium + H2O
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slow hydrolysis
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3-(acetamido)-N,N,N-trimethylanilinum + H2O
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ATMA
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?
3-methylbutyrylthiocholine + H2O
thiocholine + 3-methylbutyrate
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recombinant enzyme shows about 1% activity compared to acetylthiocholine
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?
6-monoacetylmorphine + H2O
morphine + acetate
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?
acetyl-beta-methylcholine + H2O
methylcholine + acetate
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?
acetyl-beta-methylthiocholine + H2O
beta-methylthiocholine + acetate
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acetyl-homo-thiocholine + H2O
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recombinant enzyme shows less than 10% activity compared to acetylthiocholine
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acetylcholine + H2O
acetate + choline
acetylcholine + H2O
choline + acetate
acetylthiocholine + H2O
acetate + thiocholine
acetylthiocholine + H2O
thiocholine + acetate
acetylthiocholine chloride + H2O
acetate + thiocholine chloride
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?
acetylthiocholine iodide + H2O
acetate + thiocholine iodide
acetylthiocholine iodide + H2O
thiocholine + acetate
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?
acetylthiocholine iodide + H2O
thiocholine iodide + acetate
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alpha-naphthyl acetate + H2O
alpha-naphthol + acetate
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benzoylthiocholine + H2O
thiocholine + benzoate
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recombinant enzyme shows about 1% activity compared to acetylthiocholine
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butyrylthiocholine + H2O
thiocholine + butyrate
carbachol + H2O
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slow hydrolysis
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cyclopentylcarbonylthiocholine + H2O
thiocholine + cyclopentanecarboxylate
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recombinant enzyme shows about 4% activity compared to acetylthiocholine
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cyclopropylcarbonylthiocholine + H2O
thiocholine + cyclopropanecarboxylate
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recombinant enzyme shows about 4% activity compared to acetylthiocholine
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diisopropyl phosphofluoridate + H2O
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mutant G117H, no activity with the wild-type enzyme
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echothiophate + H2O
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mutant G117H, no activity with the wild-type enzyme
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heroin + H2O
6-monoacetylmorphine + acetate
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hexanoylthiocholine + H2O
thiocholine + hexanoate
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recombinant enzyme shows about 6% activity compared to acetylthiocholine
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indophenylacetate + H2O
indophenol + acetate
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isobutyrylthiocholine + H2O
thiocholine + isobutyrate
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recombinant enzyme shows about 2% activity compared to acetylthiocholine
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paraoxon + H2O
diethylphosphate + 4-nitrophenol
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mutant G117H, no activity with the wild-type enzyme
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pentanoylthiocholine + H2O
thiocholine + pentanoate
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recombinant enzyme shows about 5% activity compared to acetylthiocholine
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phenylacetylthiocholine + H2O
thiocholine + phenylacetate
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recombinant enzyme shows about 7% activity compared to acetylthiocholine
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pivaloylthiocholine + H2O
thiocholine + pivalate
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recombinant enzyme shows about 5% activity compared to acetylthiocholine
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propionylthiocholine + H2O
thiocholine + propionate
S-acetylthiocholine + H2O
acetate + thiocholine
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detection with 5,5'-dithio-bis-2-nitrobenzoic acid, i.e. DTNB
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S-acetylthiocholine iodide + H2O
acetate + thiocholine iodide
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detection with 5,5'-dithio-bis-2-nitrobenzoic acid, i.e. DTNB
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additional information
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acetylcholine + H2O

acetate + choline
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acetylcholine + H2O
acetate + choline
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acetylcholine protects cardiomyocytes from prolonged hypoxia through activation of the PI3K/Akt/HIF-1alpha/VEGF pathway and that cardiomyocyte-derived VEGF promotes angiogenesis in a paracrine fashion
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acetylcholine + H2O

choline + acetate
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acetylcholine + H2O
choline + acetate
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acetylcholine + H2O
choline + acetate
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acetylcholine + H2O
choline + acetate
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acetylcholine + H2O
choline + acetate
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677724, 682017, 713996, 714110, 714704, 716950, 716958, 728999, 729173, 729380, 729388, 729391, 730993, 730995, 730996, 730997, 749984 -
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acetylcholine + H2O
choline + acetate
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acetylcholine + H2O
choline + acetate
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acetylcholine + H2O
choline + acetate
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acetylcholine + H2O
choline + acetate
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acetylcholine + H2O
choline + acetate
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acetylcholine + H2O
choline + acetate
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acetylcholine + H2O
choline + acetate
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acetylcholine + H2O
choline + acetate
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acetylcholine + H2O
choline + acetate
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acetylcholine + H2O
choline + acetate
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acetylcholine + H2O
choline + acetate
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acetylcholine + H2O
choline + acetate
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acetylcholine + H2O
choline + acetate
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acetylcholine + H2O
choline + acetate
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key enzyme in the central and peripheral nervous systems where it is responsible for the hydrolysis of neurotransmitter acetylcholine into choline and acetate
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acetylcholine + H2O
choline + acetate
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the enzyme might be involved in slowing of neurodegeneration in Alzheimerâs and Parkinsonâs diseases, overview
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acetylcholine + H2O
choline + acetate
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fast hydrolysis
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acetylthiocholine + H2O

acetate + thiocholine
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acetylthiocholine + H2O
acetate + thiocholine
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detection using 5,5'-dithiobis(2-nitrobenzoic acid)
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acetylthiocholine + H2O

thiocholine + acetate
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acetylthiocholine + H2O
thiocholine + acetate
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acetylthiocholine + H2O
thiocholine + acetate
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acetylthiocholine + H2O
thiocholine + acetate
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acetylthiocholine + H2O
thiocholine + acetate
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acetylthiocholine + H2O
thiocholine + acetate
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acetylthiocholine + H2O
thiocholine + acetate
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664578, 677724, 677953, 678096, 678101, 678228, 678404, 679202, 680235, 681108, 682017, 682920, 682921, 714852, 728999, 729388, 729391, 730993, 730995, 730996, 730997, 749984 -
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acetylthiocholine + H2O
thiocholine + acetate
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acetylthiocholine + H2O
thiocholine + acetate
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acetylthiocholine + H2O
thiocholine + acetate
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acetylthiocholine + H2O
thiocholine + acetate
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acetylthiocholine + H2O
thiocholine + acetate
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acetylthiocholine + H2O
thiocholine + acetate
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acetylthiocholine + H2O
thiocholine + acetate
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acetylthiocholine + H2O
thiocholine + acetate
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best substrate
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acetylthiocholine + H2O
thiocholine + acetate
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100% activity
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acetylthiocholine + H2O
thiocholine + acetate
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fast hydrolysis
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acetylthiocholine + H2O
thiocholine + acetate
activity of AChE is determined by Ellman's method using acetylthiocholine iodide as a substrate
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acetylthiocholine + H2O
thiocholine + acetate
substrate is acetylthiocholine iodide
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acetylthiocholine + H2O
thiocholine + acetate
substrate is acetylthiocholine iodide, activity detection using 5,5'-dithio-bis(2-nitrobenzoic acid) colorimetric assay and measurement of the absorbance at 412 nm
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acetylthiocholine + H2O
thiocholine + acetate
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substrate is acetylthiocholine iodide, activity detection using 5,5'-dithio-bis(2-nitrobenzoic acid) colorimetric assay and measurement of the absorbance at 412 nm
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acetylthiocholine iodide + H2O

acetate + thiocholine iodide
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acetylthiocholine iodide + H2O
acetate + thiocholine iodide
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acetylthiocholine iodide + H2O
acetate + thiocholine iodide
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detection with 5,5'-dithio-bis-2-nitrobenzoic acid, i.e. DTNB
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butyrylthiocholine + H2O

thiocholine + butyrate
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butyrylthiocholine + H2O
thiocholine + butyrate
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recombinant enzyme shows about 3% activity compared to acetylthiocholine
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propionylthiocholine + H2O

thiocholine + propionate
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propionylthiocholine + H2O
thiocholine + propionate
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propionylthiocholine + H2O
thiocholine + propionate
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recombinant enzyme shows about 52% activity compared to acetylthiocholine
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additional information

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additional information
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pivotal role in the cholinergic system, rapid termination of nerve impulse transmission
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additional information
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calcium-activated BuchE, EC 3.1.1.8, acts as a major protective mechanism against suicide inhibition of AchE by organophosphates in this non-neuronal tissue, overview
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additional information
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the reactivation of nerve agent-inhibited acetylcholinesterase by oxime is the most important step in the treatment of nerve agent poisoning, overview
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additional information
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acetylcholinesterase is a serine hydrolase that catalyze the hydrolysis of acetylcholine, thus regulating cholinergic neurotransmission
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additional information
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inhibition of AChE, along with the butyrylcholinesterase, and restoration of acetylcholine is a therapeutic strategy in treatment of Alzheimer's disease and other forms of dementia
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additional information
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bioassay for inhibition of fibril formation, i.e. Thioflavin T assay
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additional information
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the ensemble of compound 1 and compound 2 can be used for the AChE activity assay and the inhibitor-screening by making use of the aggregation-induced emission feature of tetraphenyl ethylene compounds, method development, overview
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additional information
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interactions between acetylcholinesterase, toxic organophosphorus compounds and a short series of structurally related non-oxime reactivators, analysis of reactivation and inhibition kinetics in vitro, overview
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additional information
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interactions between acetylcholinesterase, toxic organophosphorus compounds and a short series of structurally related non-oxime reactivators, analysis of reactivation and inhibition kinetics in vitro, overview
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additional information
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no activity with butyrylcholine
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additional information
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nonspecific inhibitor neostigmine is used to inhibit hemolysate AChE activity in order to understand the specificity of AChE for 1-naphthyl acetate or acetylthiocholine, substrate docking with AChE, BChE (EC 3.1.1.8), albumin and esterase D, acetylcholine docks with AChE, BChE, albumin and esterase D, overview
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additional information
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substrate specificities of AChE compared to butyrylcholinesterase (EC 3.1.1.8) and cocaine esterase (EC 3.1.1.84)
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additional information
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the acetylcholinesterase (AChE) enzyme activity is detected using the 5,5'-dithio-bis(2-nitrobenzoic acid)-based colorimetric assay with measurement of the absorbance at 412 nm. 2,6-Dichloroindophenol acetate is performed as a chromogenic substrate also suitable for AChE activity examination
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additional information
?
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the acetylcholinesterase (AChE) enzyme activity is detected using the 5,5'-dithio-bis(2-nitrobenzoic acid)-based colorimetric assay with measurement of the absorbance at 412 nm. 2,6-Dichloroindophenol acetate is performed as a chromogenic substrate also suitable for AChE activity examination
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?
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