Kask K, Berthold M, Bartfai T
Department of Neurochemistry and Neurotoxicology, Stockholm University, Sweden.
Life Sci. 1997;60(18):1523-33. doi: 10.1016/s0024-3205(96)00624-8.
Galanin, a neuroendocrine peptide with a multitude of functions, binds to and acts on specific G-protein coupled receptors. Only one galanin receptor subtype, GalRI, has been cloned so far, although pharmacological evidence suggests the presence of more than one galanin receptor subtype. These receptors mediate via different Gi/Go-proteins the inhibition of adenylyl cyclase, opening of K+-channels and closure of Ca2+-channels. Galanin inhibits secretion of insulin, acetylcholine, serotonin and noradrenaline, while it stimulates prolactin and growth hormone release. Determination of structural components of galanin receptors required for binding of the peptide ligand as carried out recently will facilitate the screening and design of molecules specifically acting on galaninergic systems with therapeutic potential in Alzheimer's disease, feeding disorders, pain and depression.
甘丙肽是一种具有多种功能的神经内分泌肽,它与特定的G蛋白偶联受体结合并发挥作用。尽管药理学证据表明存在不止一种甘丙肽受体亚型,但迄今为止仅克隆出一种甘丙肽受体亚型GalRI。这些受体通过不同的Gi/Go蛋白介导腺苷酸环化酶的抑制、钾通道的开放和钙通道的关闭。甘丙肽抑制胰岛素、乙酰胆碱、5-羟色胺和去甲肾上腺素的分泌,同时刺激催乳素和生长激素的释放。最近对肽配体结合所需的甘丙肽受体结构成分的测定,将有助于筛选和设计特异性作用于甘丙肽能系统的分子,这些分子在阿尔茨海默病、进食障碍、疼痛和抑郁症方面具有治疗潜力。