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Trends Pharmacol Sci. 1992 Dec;13(12):446-50.

GABAA receptors: ligand-gated Cl- ion channels modulated by multiple drug-binding sites.

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Department of Biochemical Psychiatry, University Clinic for Psychiatry, Vienna, Austria.


GABAA receptors are ligand-gated Cl- ion channels and the site of action of a variety of pharmacologically and clinically important drugs. In this review evidence is summarized indicating that these drugs, by interacting with several distinct binding sites at these receptors, allosterically modulate GABA-induced Cl- ion flux. Other results indicate that the affinity, as well as the modulatory efficacy of drugs, changes with receptor composition. A though investigation of the pharmacological properties of the individual binding sites on different GABAA receptor subtypes could open new avenues for selective modulation of GABAA receptors in different brain regions.

[Indexed for MEDLINE]

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