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The Muscarinic Acetylcholine Receptor M5: Therapeutic Implications and Allosteric Modulation
ACS Chemical Neuroscience ( IF 5 ) Pub Date : 2018-10-03 00:00:00 , DOI: 10.1021/acschemneuro.8b00481
Aaron M. Bender 1, 2 , Aaron T. Garrison 1, 2 , Craig W. Lindsley 1, 2
Affiliation  

The muscarinic acetylcholine receptor (mAChR) subtype 5 (M5) was the most recent mAChR to be cloned and has since emerged as a potential therapeutic target for a number of indications. Early studies with knockout animals have provided clues to the receptor’s role in physiological processes related to Alzheimer’s disease, schizophrenia, and addiction, and until recently, useful subtype-selective tools to further probe the pharmacology of M5 have remained elusive. Small-molecule allosteric modulators have since gained traction as a means by which to selectively examine muscarinic pharmacology. This review highlights the discovery and optimization of M5 positive allosteric modulators (PAMs) and negative allosteric modulators (NAMs).

中文翻译:

毒蕈碱型乙酰胆碱受体M 5:治疗意义和变构调节。

毒蕈碱型乙酰胆碱受体(mAChR)5亚型(M 5)是最近被克隆的mAChR,此后已成为许多适应症的潜在治疗靶标。早期对基因敲除动物的研究提供了有关受体在与阿尔茨海默氏病,精神分裂症和成瘾有关的生理过程中的作用的线索,直到最近,用于进一步探查M 5药理学的有用的亚型选择性工具仍然难以捉摸。此后,小分子变构调节剂获得了牵引力,以此作为选择性检查毒蕈碱药理学的手段。这篇综述重点介绍了M 5正构构调节剂(PAM)和负构构调节剂(NAM)的发现和优化。
更新日期:2018-10-03
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