Action of Organophosphate Anticholinesterases on the Three Conformational States of Nicotinic Receptor
Organophosphate and other ligands were examined for binding on the membrane-bond nicotinic receptor at three conformational states. Soman (pinacolyl methylphosphonofluoridate), sarin (isopropyl methylphosphonofluoridate, tabun (ethyl N-dimethylphosphoramidocyanidate) and phencyclidine did not show any effect on the binding of [25I]α-cobrotoxin to the nicotinic receptor. However, VX, O-ethyl-S-(2-diisopropylaminoethyl) methylphosphonothiolate, at concentrations higher than 10 umol/L exhibited profound inhibition on the equilibrium binding rates in a concentration-dependent manner. Agonist nicotine and antagonist d-tubocurarine also showed significant inhibitions.
KeywordsNicotinic Receptor Conformational State Total Binding Electric Organ Binding Rate
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