Progress in α5GABAA receptors and their allosteric modulators in learning-memory / 中国药理学与毒理学杂志

ABSTRACT

Alpha 5 subunit-containing γ-aminobutyric acid type A receptors (α5GABAARs), mainly distributed in the hippocampus, are an inhibitory synaptic receptor of the central nervous system.α5GABAARs inhibit the hippocampal neurons by mediating a chloride leak current. A number of studies have demonstrated that alterations in the level of excitability of α5GABAARs impair cognitive function and learning-memory, thus resulting in a series of diseases and symptoms including postoperative cognitive dysfunction, pain, depression, schizophrenia and Down syndrome. Accordingly, allosteric modulators for α5GABAARs show therapeutic or improving effects on the above clinical diseases. This review mainly discusses the physiology of α5GABAARs, impact on cognition and key effects of these allosteric modulators.