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Direct action of ethanol on cerebral gaba a receptor complex analysis using purified and reconstituted gaba a receptor complex



Direct action of ethanol on cerebral gaba a receptor complex analysis using purified and reconstituted gaba a receptor complex



Neurochemistry International 19(3): 319-326



Possible direct action of ethanol on cerebral GABAA receptor complex has been analyzed using reconstituted vesicles with purified GABAA/benzodiazepine receptor/Cl ion channel complex prepared from the bovine cerebral cortex. Addition of ethanol to the reconstituted vesicles with purified GABAA receptor complex induced a significant facilitation of GABA-dependent 36Cl- influx in a dose-dependent manner. Furthermore, the reconstituted vesicles with pretreated GABAA receptor complex with 20 mM ethanol, a dose that had no significant effect on GABAA receptor binding, also exhibited a significant increase of GABA-dependent 36Cl- influx as compared with that found in non-treated preparation. On the other hand, the facilitation of GABA-dependent 36Cl- influx by flunitrazepam was found to be eliminated by the ethanol pretreatment. The present results suggest that ethanol may affect directly on GABAA receptor complex and facilitate the function of Cl ion channel but eliminate or decrease the functional coupling between benzodiazepine receptor and GABAA receptor.

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