The Effects of Chronic Ethanol Intake on the Allosteric Interaction Between GABA and Benzodiazepine at the GABAA Receptor (open access)

The Effects of Chronic Ethanol Intake on the Allosteric Interaction Between GABA and Benzodiazepine at the GABAA Receptor

This study examined the effects of chronic ethanol intake on the density, affinity, and allosteric modulation of rat brain GABAA receptor subtypes. In the presence of GABA, the apparent affinity for the benzodiazepine agonist flunitrazepam was increased and for the inverse agonist R015-4513 was decreased. No alteration in the capacity of GABA to modulate flunitrazepam and R015-4513 binding was observed in membranes prepared from cortex, hippocampus or cerebellum following chronic ethanol intake or withdrawal. The results also demonstrate two different binding sites for [3H]RO 15-4513 in rat cerebellum that differ in their affinities for diazepam. Chronic ethanol treatment and withdrawal did not significantly change the apparent affinity or density of these two receptor subtypes.
Date: May 1992
Creator: Chen, Jianping
System: The UNT Digital Library