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Ethanol‐induced inhibition of a neuronal P2X purinoceptor by an allosteric mechanism
Author(s) -
Li Chaoying,
Peoples Robert W,
Weight Forrest F
Publication year - 1998
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1038/sj.bjp.0701599
Subject(s) - allosteric regulation , bullfrog , chemistry , biophysics , mechanism of action , ethanol , agonist , ion channel , neurotransmitter , electrophysiology , pharmacology , biochemistry , neuroscience , endocrinology , receptor , biology , in vitro
Ethanol inhibits a neuronal P2X purinoceptor by shifting the ATP concentration–response curve to the right in an apparently competitive manner. However, the underlying mechanism has not been determined. We investigated the effects of ethanol on the activation and deactivation time constants for ATP‐activated current in bullfrog dorsal root ganglion neurones. Ethanol decreased the time constant of deactivation of ATP‐gated ion channels without affecting the time constant of activation. The observations are not consistent with a competitive mechanism of inhibition by ethanol, but may be explained by an allosteric action of ethanol to decrease apparent agonist affinity. This represents a novel mechanism of action of ethanol on a neurotransmitter‐gated ion channel. British Journal of Pharmacology (1998) 123 , 1–3; doi: 10.1038/sj.bjp.0701599