Kerr D I, Ong J
Department of Anaesthesia and Intensive Care, University of Adelaide, Australia.
Pharmacol Ther. 1995;67(2):187-246. doi: 10.1016/0163-7258(95)00016-a.
GABAB receptors are a distinct subclass of receptors for the major inhibitory transmitter 4-aminobutanoic acid (GABA) that mediate depression of synaptic transmission and contribute to the inhibition controlling neuronal excitability. The development of specific agonists and antagonists for these receptors has led to a better understanding of their physiology and pharmacology, highlighting their diverse coupling to different intracellular effectors through Gi/G(o) proteins. This review emphasises our current knowledge of the neurophysiology and neurochemistry of GABAB receptors, including their heterogeneity, as well as the therapeutic potential of drugs acting at these sites.
GABAB受体是主要抑制性神经递质4-氨基丁酸(GABA)的一类独特的受体亚类,介导突触传递的抑制作用,并参与控制神经元兴奋性的抑制过程。针对这些受体的特异性激动剂和拮抗剂的开发,使人们对其生理学和药理学有了更好的理解,突出了它们通过Gi/G(o)蛋白与不同细胞内效应器的多样偶联。这篇综述着重阐述了我们目前对GABAB受体的神经生理学和神经化学的认识,包括其异质性,以及作用于这些位点的药物的治疗潜力。