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ＧＡＢＡＡ受体是中枢神经内最重要的抑制性受体，苯二氮艹卓类和巴比妥类均作用于ＧＡＢＡＡ受体而发挥其镇静、催眠、抗惊厥等药理作用。ＧＡＢＡＡ受体分子由５个亚单位组成，已发现的亚单位有６类１９种，这些亚单位构成脑内ＧＡＢＡＡ受体众多亚型的复杂分布。不同受体亚型的生理功能亦存在很大差异。
GABAA receptor is the most important central nervous system inhibitory receptor, benzodiazepines and barbiturates are acting on the GABAA receptor and exert its sedative, hypnotic, anticonvulsant and other pharmacological effects. The GABAA receptor molecule consists of five subunits, six of which are found in 19 subtypes, and these subunits constitute a complex distribution of numerous subtypes of GABAA receptors in the brain. Physiological functions of different receptor subtypes also vary greatly.