Pharmacological Profile of the 5-HT2C Receptor Agonist WAY-163909; Therapeutic Potential in Multiple Indications

John Dunlop, Karen L. Marquis, HK Lim, Louis Leung, John Kao, Cynthia Cheesman, Sharon Rosenzweig-Lipson
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引用次数: 73

Abstract

The 5-HT2C receptor subtype has been implicated in a wide variety of conditions including obesity, anxiety, depression, obsessive compulsive disorder, schizophrenia, migraine and erectile dysfunction and as a consequence has received considerable attention as a target for drug discovery. Here we review the pharmacological, pharmacokinetic and toxicological profile of WAY-163909 {(7bR,10aR)-1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopenta-[b][1,4]diazepino[6,7,1hi]indole}, a novel 5-HT2C receptor selective agonist. Consistent with a potential therapeutic utility in obesity, schizophrenia and depression WAY-163909 was found to have robust dose-dependent effects in animal models of obesity, psychotic-like behavior or depression.

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5-HT2C受体激动剂WAY-163909的药理学研究多种适应症的治疗潜力
5-HT2C受体亚型与多种疾病有关,包括肥胖、焦虑、抑郁、强迫症、精神分裂症、偏头痛和勃起功能障碍,因此作为药物发现的靶点受到了相当大的关注。本文综述了一种新型5-HT2C受体选择性激动剂WAY-163909 {(7bR,10aR)-1,2,3,4,8,9,10,10 - a-八氢- 7hb -环五氢-[b][1,4]diazepino[6,7,1hi]吲哚}的药理学、药代动力学和毒理学特征。与肥胖、精神分裂症和抑郁症的潜在治疗效用一致,WAY-163909被发现在肥胖、精神病样行为或抑郁症的动物模型中具有强大的剂量依赖效应。
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