Abstract
Organophosphorus and carbamate insecticides are toxic to insects and mammals by virtue of their ability to inactivate the enzyme acetylcholinesterase. This review addresses the mechanism of inhibition of acetylcholinesterase by organophosphorus and carbamate esters, focusing on structural requirements necessary for anticholinesterase activity. The inhibition of acetylcholinesterase by these compounds is discussed in terms of reactivity and steric effects. The role of metabolic activation or degradation in the overall intoxication process is also discussed.
MeSH terms
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Animals
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Biotransformation
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Carbamates*
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Cholinesterase Inhibitors / chemistry
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Cholinesterase Inhibitors / pharmacokinetics
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Cholinesterase Inhibitors / toxicity*
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Inactivation, Metabolic
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Insecta
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Insecticides / chemistry
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Insecticides / pharmacokinetics
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Insecticides / toxicity*
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Mammals
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Mixed Function Oxygenases / metabolism
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Molecular Structure
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Organophosphorus Compounds*
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Oxidation-Reduction
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Structure-Activity Relationship
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Synaptic Transmission / drug effects
Substances
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Carbamates
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Cholinesterase Inhibitors
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Insecticides
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Organophosphorus Compounds
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Mixed Function Oxygenases