Ligand-dependent effects of ethanol and diethylether at brain benzodiazepine receptors

Pharmacology, Biochemistry, and Behavior
J J Quinlan, L L Firestone


The GABAA receptor chloride channel complex interacts with various categories of sedatives, including the benzodiazepines, and possibly ethanol and volatile general anesthetics. Thus, specific binding of tritiated derivatives of a benzodiazepine antagonist, flumazenil, and an agonist, flunitrazepam, to rat brain membrane fragments was monitored at equilibrium in the presence and absence of anesthetizing concentrations of ethanol and diethylether. Ethanol produced a concentration-dependent inhibition of [3H]flumazenil binding, which was not reversed by the GABAA receptor competitive antagonist bicuculline, but had no effect on [3H]flunitrazepam binding. Both ethanol and diethylether decreased the affinity of the benzodiazepine site for [3H]flumazenil. These data indicate that ethanol and diethylether have GABA-independent effects at the benzodiazepine sites of the GABAA receptor. These findings are inconsistent with a two-state functional model of the benzodiazepine site and, instead, support a model containing a specific, antagonist-favored conformation.


Apr 21, 1977·Nature·R F Squires, C Brastrup
Jun 1, 1986·Proceedings of the National Academy of Sciences of the United States of America·P D SuzdakS M Paul
May 1, 1987·Medical Hypotheses·S C Cheng, E A Brunner
Dec 30, 1983·Neuroscience Letters·J H Skerritt, R L Macdonald
Dec 24, 1981·Nature·H Möhler, J G Richards
Apr 1, 1984·Journal of Neurochemistry·D A GreenbergI Diamond

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Tissue Membrane
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