Astraea Therapeutics, LLC. 320 Logue Avenue, Mountain View, CA 94043, United States.
Life Sci. 2013 Mar 19;92(8-9):425-37. doi: 10.1016/j.lfs.2012.10.032. Epub 2012 Nov 16.
Since the discovery of the TRPM8 gene in 2001, the TRPM8 ion channel, better known as the 'cold receptor' has been the target of a significant effort from the pharmaceutical industry to produce small-molecule agonists and antagonists of this receptor for various therapeutic applications ranging from cancer and urological disorders to the treatment of cold hypersensitivity and pain. Recently, a number of clinical studies have implicated menthol, the natural ligand of TRPM8, in facilitating and maintaining cigarette smoking behavior, possibly through its counter-irritant effects. However, a pharmacological link between menthol's action via TRPM8 and nicotine addiction has not been yet been investigated. This review gives an overview of reported small-molecule TRPM8 agonists and antagonists and discusses their efficacy in models of various disease states. These compounds may be useful pharmacological tools to investigate the effect of menthol on nicotine addiction.
自 2001 年发现 TRPM8 基因以来，TRPM8 离子通道，更为人所知的是“冷受体”，一直是制药行业的研究目标，旨在针对该受体开发小分子激动剂和拮抗剂，用于各种治疗应用，从癌症和泌尿系统疾病到治疗冷过敏和疼痛。最近，许多临床研究表明，薄荷醇，TRPM8 的天然配体，可能通过其抗刺激作用，促进和维持吸烟行为。然而，薄荷醇通过 TRPM8 发挥作用与尼古丁成瘾之间的药理联系尚未得到研究。这篇综述概述了已报道的小分子 TRPM8 激动剂和拮抗剂，并讨论了它们在各种疾病模型中的疗效。这些化合物可能是研究薄荷醇对尼古丁成瘾影响的有用药理学工具。
