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黑色素聚集激素在神经系统中的作用:食物摄入与应激。

Melanin-concentrating hormone functions in the nervous system: food intake and stress.

作者信息

Hervieu Guillaume

机构信息

GlaxoSmithKline R&D, Drug Discovery, Neurology Centre of Excellence for Drug Discovery, New Frontiers Science Park - North, HW1713 Building H17, L1-130 C06 Third Avenue, Harlow, Essex CM19 5AW, UK.

出版信息

Expert Opin Ther Targets. 2003 Aug;7(4):495-511. doi: 10.1517/14728222.7.4.495.

Abstract

Melanin-concentrating hormone (MCH) is a cyclic neuropeptide, which centrally regulates food intake and stress. MCH induces food intake in rodents and, more generally, acts as an anabolic signal in energy regulation. In addition, MCH seems to be activatory on the stress axis. Two receptors for MCH in humans have very recently been characterised, namely, MCH-R1 and MCH-R2. MCH-R1 has received considerable attention, as potent and selective antagonists acting at that receptor display anxiolytic, antidepressant and/or anorectic properties. Feeding and affective disorders are both debilitating conditions that have become serious worldwide health threats. There are as yet no efficient and/or safe cures that could contain the near-pandemia phenomen of both diseases. Thus, the discovery of MCH-R1 antagonists may lead to the development of valuable drugs to treat obesity, anxiety and depressive syndromes. In addition, it opens wide avenues to probe additional functions of the peptide, both in the brain and in the peripheral nervous system.

摘要

促黑素细胞激素(MCH)是一种环状神经肽,可在中枢调节食物摄入和应激反应。MCH可诱导啮齿动物进食,更广泛地说,它在能量调节中作为一种合成代谢信号发挥作用。此外,MCH似乎对应激轴具有激活作用。最近已鉴定出人类体内的两种MCH受体,即MCH-R1和MCH-R2。MCH-R1受到了相当多的关注,因为作用于该受体的强效选择性拮抗剂具有抗焦虑、抗抑郁和/或厌食特性。饮食和情感障碍都是使人衰弱的病症,已成为全球严重的健康威胁。目前尚无有效和/或安全的疗法能够控制这两种疾病近乎大流行的现象。因此,MCH-R1拮抗剂的发现可能会推动开发出治疗肥胖症、焦虑症和抑郁症综合征的有价值药物。此外,它还为探究该肽在大脑和外周神经系统中的其他功能开辟了广阔途径。

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