Molecular pharmacology
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Molecular pharmacology · Oct 2001
The kinetics of competitive antagonism by cisatracurium of embryonic and adult nicotinic acetylcholine receptors.
Competitive antagonists to nicotinic acetylcholine receptors are clinically used as muscle relaxants. Previously, we reported the kinetics of inhibition (in the absence of acetylcholine) by (+)-tubocurarine and pancuronium on embryonic receptors. Here, we examine cisatracurium, a commonly used muscle relaxant. ⋯ These data suggest that presence of acetylcholine on one binding site of the receptor increases the dissociation rate of antagonist from the other binding site. We incorporated all of these rates into a computer simulation of a comprehensive 11-state Markov model. There was excellent agreement (without curve fitting) between simulated and experimental currents.