GABA A receptor subtypes: from pharmacology to molecular biology

Abstract

GABA A receptors are GABA (γ‐amino‐butyric acid)‐gated chloride channels, which are major mediators of neuronal inhibition in the brain and are modulated by benzodiazepines, barbiturates, alcohol, and other important centrally acting drugs. Although previous pharmacological and biochemical data had suggested a degree of heterogeneity, recent cloning of at least 15 different receptor subunits, thought to be combined in groups of five, indicates that the brain may contain a truly astonishing variety of GABA a receptor subtypes. This review describes the little that is known about these subtypes, emphasizing possible molecular bases of receptor heterogeneity. We also discuss approaches to establishing the subunit composition of subtypes.—Burt, D. R.; Kamatchi, G. L. GABA A receptor subtypes: from pharmacology to molecular biology. FASEB J. 5: 2916‐2923; 1991.