Pritchett D B, Sontheimer H, Gorman C M, Kettenmann H, Seeburg P H, Schofield P R
Laboratory of Molecular Neuroendocrinology, ZMBH, University of Heidelberg, Federal Republic of Germany.
Science. 1988 Dec 2;242(4883):1306-8. doi: 10.1126/science.2848320.
Human gamma-aminobutyric acid A (GABAA) receptor subunits were expressed transiently in cultured mammalian cells. This expression system allows the simultaneous characterization of ligand-gated ion channels by electrophysiology and by pharmacology. Thus, coexpression of the alpha and beta subunits of the GABAA receptor generated GABA-gated chloride channels and binding sites for GABAA receptor ligands. Channels consisting of only alpha or beta subunits could also be detected. These homomeric channels formed with reduced efficiencies compared to the heteromeric receptors. Both of these homomeric GABA-responsive channels were potentiated by barbiturate, indicating that sites for both ligand-gating and allosteric potentiation are present on receptors assembled from either subunit.
人类γ-氨基丁酸A（GABAA）受体亚基在培养的哺乳动物细胞中瞬时表达。该表达系统允许通过电生理学和药理学同时表征配体门控离子通道。因此，GABAA受体的α和β亚基的共表达产生了GABA门控氯离子通道和GABAA受体配体的结合位点。仅由α或β亚基组成的通道也可以被检测到。与异源受体相比，这些同源通道形成的效率较低。这两种同源GABA反应性通道都被巴比妥酸盐增强，表明配体门控和变构增强的位点都存在于由任何一个亚基组装而成的受体上。
