GABA receptor activation

Gamma aminobutyric acid (GABA) receptors are the major inhibitory receptors in human synapses. They are of two types. GABA A receptors are fast-acting ligand gated chloride ion channels that mediate membrane depolarization and thus inhibit neurotransmitter release (G Michels et al Crit Rev Biochem Mol Biol 42, 2007, 3-14). GABA B receptors are slow acting metabotropic Gprotein coupled receptors that act via the inhibitory action of their Galpha/Go subunits on adenylate cyclase to attenuate the actions of PKA. In addition, their Gbeta/gamma subunits interact directly with N and P/Q Ca2+ channels to decrease the release of Ca2+. GABA B receptors also interact with Kir3 K+ channels and increase the influx of K+, leading to cell membrane hyperpolarization and inhibition of channels such as NMDA receptors (A Pinard et al Adv Pharmacol, 58, 2010, 231-55).

γ-氨基丁酸（GABA）受体是人类突触中的主要抑制性受体。它们分为两种类型。GABA A 受体为快速作用的配体门控氯离子通道，介导膜去极化，从而抑制神经递质的释放（G Michels 等人，生物化学与分子生物学评论，42，2007，3-14）。GABA B 受体为缓慢作用的代谢型 G 蛋白偶联受体，通过其 Galpha/Go 亚基对腺苷酸环化酶的抑制性作用来减弱 PKA 的活性。此外，它们的 Gbeta/gamma 亚基直接与 N 和 P/Q 型 Ca2+ 通道相互作用，以减少 Ca2+ 的释放。GABA B 受体还与 Kir3 K+ 通道相互作用，增加 K+ 的内流，导致细胞膜超极化，并抑制如 NMDA 受体等通道（A Pinard 等人，药物学进展，58，2010，231-55）。