Burt D R, Kamatchi G L
Department of Pharmacology and Experimental Therapeutics, University of Maryland School of Medicine, Baltimore 21201.
FASEB J. 1991 Nov;5(14):2916-23. doi: 10.1096/fasebj.5.14.1661244.
GABAA receptors are GABA (gamma-aminobutyric 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 GABAA 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.
GABAA受体是γ-氨基丁酸（GABA）门控的氯离子通道，是大脑中神经元抑制的主要介质，并且受到苯二氮䓬类、巴比妥类、酒精及其他重要的中枢作用药物的调节。尽管先前的药理学和生化数据表明存在一定程度的异质性，但最近克隆出至少15种不同的受体亚基（据认为以五个一组进行组合），这表明大脑中可能含有种类惊人的GABAA受体亚型。这篇综述描述了对这些亚型所知甚少的情况，着重强调受体异质性可能的分子基础。我们还讨论了确定亚型亚基组成的方法。
