Mechanisms of Action of Anticholinesterases and Oximes on Acetylcholine Receptors

Abstract

Oximes are strong nucleophiles, capable of activating phosphorylated acetylcholine (ACh)-esterase. In this report we provide evidence that, in addition to their action on the enzyme, oximes also react with nicotinic and muscarinic receptors. In our studies, we found 2-PAM, HI-6, and Toxogonin bound to both nicotinic and muscarinic ACh receptors. Modulation of binding of nicotinic receptor ligands in the Torpedo electric organ suggested that the oximes acted as nicotinic receptor antagonists. Inhibition of the receptor- regulated 22Na+ transport supported this conclusion. These three oximes also bound to muscarinic ACh receptors of rat brain and displaced receptor agonists (e.g., (3H)CD) and antagonists (e.g., (3H)QNB and (3H)PZ). Keywords: Nicotinic and muscarinic acetylcholine receptors; Oximes; Binding of radioactive receptor ligands.

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Document Details

Document Type
Technical Report
Publication Date
Jul 23, 1988
Accession Number
ADA223952

Entities

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  • Mohyee E. Eldefrawi

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  • University of Maryland School of Medicine

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  • Biomedical

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