γ-氨基丁酸受体
γ-氨基丁酸受体
受体
蛋白质亚单位
半胱氨酸环受体
加巴能
生物
生物化学
神经科学
细胞生物学
生物物理学
乙酰胆碱受体
基因
烟碱乙酰胆碱受体
作者
Werner Sieghart,Karoline Fuchs,Verena Tretter,Veronika Ebert,Martin Jechlinger,Harald Höger,D. Adamiker
标识
DOI:10.1016/s0197-0186(99)00045-5
摘要
GABAA receptors are the major inhibitory neurotransmitter receptors in the brain and are the site of action of many clinically important drugs. These receptors are composed of five subunits that can belong to eight different subunit classes. If all GABAA receptor subunits could randomly combine with each other, an extremely large number of GABAA receptor subtypes with distinct subunit composition and arrangement would be formed. Depending on their subunit composition, these receptors would exhibit distinct pharmacological and electrophysiological properties. Recent evidence, however, indicates that not all subunits can assemble efficiently with each other and form functional homo- or hetero-oligomeric receptors. In addition, the efficiency of formation of hetero-oligomeric assembly intermediates determines the subunit stoichiometry and subunit arrangement for each receptor and thus further reduces the possible heterogeneity of GABAA receptors in the brain. Studies investigating the subunit composition of native GABAA receptors support this conclusion, but also indicate that receptors composed of one, two, three, four, or five different subunits might exist in the brain. Using a recently established immunodepletion technique, the subunit composition and quantitative importance of native GABAA receptor subtypes can be determined. This information, together with studies on the regional, cellular and subcellular distribution of these receptor subtypes, will be the basis for a rational development of drugs that specifically affect the GABAergic system.
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