Li De-Pei, Pan Hui-Lin
Department of Critical Care, The University of Texas, M. D. Anderson Cancer Center, Houston, Texas, USA.
Adv Pharmacol. 2010;58:257-86. doi: 10.1016/S1054-3589(10)58011-6.
GABA(B) receptors belong to family III G protein-coupled receptors (GPCRs) and are widely distributed in the peripheral and central nervous systems. The GABA(B) receptor is one of the most important therapeutic targets in the treatment for spasticity. GABA(B) agonists, such as baclofen, are used as muscle relaxants clinically and are effective for the treatment of anxiety, depression, epilepsy, and cognitive disorders (Caddick & Hosford, 1996; Dichter, 1997; Enna & Bowery, 1997). In addition, GABA(B) receptors regulate neurotransmitter release and neuronal excitability in the brain regions involved in the autonomic nervous system. Recent studies have led to a better understanding of the role of GABA(B) in the regulation of the autonomic nervous system, especially in disease conditions such as hypertension. Here, we provide an overview of the recent progress, a discussion of disparate and contradictory findings, and a description of theories used to explain various cardiovascular effects of GABA(B) receptor drugs. Particular emphasis is placed on the role of GABA(B) receptors in the neural plasticity of brain regions related to the control of sympathetic outflow in cardiovascular disorders.
γ-氨基丁酸B(GABA(B))受体属于III类G蛋白偶联受体(GPCRs),广泛分布于外周和中枢神经系统。GABA(B)受体是治疗痉挛最重要的治疗靶点之一。GABA(B)激动剂,如巴氯芬,在临床上用作肌肉松弛剂,对治疗焦虑、抑郁、癫痫和认知障碍有效(Caddick和Hosford,1996年;Dichter,1997年;Enna和Bowery,1997年)。此外,GABA(B)受体调节参与自主神经系统的脑区中的神经递质释放和神经元兴奋性。最近的研究使人们对GABA(B)在自主神经系统调节中的作用有了更好的理解,尤其是在高血压等疾病状态下。在此,我们概述了最近的进展,讨论了不同和矛盾的发现,并描述了用于解释GABA(B)受体药物各种心血管效应的理论。特别强调了GABA(B)受体在与心血管疾病中交感神经流出控制相关的脑区神经可塑性中的作用。