Fukuda H, Ito Y
College of Pharmacy, Nihon University, Chiba, Japan.
Yakugaku Zasshi. 1998 Sep;118(9):339-52. doi: 10.1248/yakushi1947.118.9_339.
gamma-Aminobutyric acid (GABA) is a major inhibitory neurotransmitter in the central nervous system. GABA receptors have been classified into at least two categories, GABA(A) receptors, which are heterogeneous multimeric ligand-gated Cl channels, and GABA(B) receptors, which are coupled to G-proteins. GABA(B) receptors have not only a physiological role in synaptic transmission, but also are important in pathological conditions associated with absence epilepsy, cognitive disorders and nociception. This review describes our current knowledge of the neuropharmacology and neurochemistry of GABA(B) receptors, including their heterogeneity as well as the therapeutic potential of the drugs which interact with these sites.
γ-氨基丁酸（GABA）是中枢神经系统中的一种主要抑制性神经递质。GABA受体至少已被分为两类，即GABA(A)受体和GABA(B)受体，前者是异源多聚体配体门控氯离子通道，后者与G蛋白偶联。GABA(B)受体不仅在突触传递中具有生理作用，而且在与失神癫痫、认知障碍和痛觉感受相关的病理状况中也很重要。本综述描述了我们目前对GABA(B)受体的神经药理学和神经化学的认识，包括它们的异质性以及与这些位点相互作用的药物的治疗潜力。
