Dipartimento Farmaco Chimico Tecnologico and European Research Centre for Drug Discovery and Development, Università di Siena, Via A. Moro, 53100 Siena, Italy.
Curr Top Med Chem. 2010;10(5):504-26. doi: 10.2174/156802610791111560.
The 5-HT(3) receptor (5-HT(3)R) occupies a special place among the serotonin receptor subtypes because it has been shown to be a ligand-gated ion channel, which is involved in a number of physiological functions and important pathologies. 5-HT(3)R antagonists have shown an outstanding efficacy in the control of the emesis induced by anticancer chemotherapy and few adverse side-effects, so as to revolutionize the treatment of nausea in cancer patients. This review covers the authors' work performed during the past decade in the development of 5-HT(3)R ligands belonging to the class of arylpiperazine derivatives related to quipazine (quipazine-like arylpiperazines, QLAs) and represents the extension of the review previously published in Current Topics in Medicinal Chemistry in 2002. The discussion is focused mainly on the most significant structure-affinity relationships emerged in the progress of the work and shows how the original ideas have evolved in the recent years.
5-羟色胺（3）受体（5-HT（3）R）在血清素受体亚型中占有特殊地位，因为它已被证明是一种配体门控离子通道，参与许多生理功能和重要的病理过程。5-HT（3）R 拮抗剂在控制抗癌化疗引起的呕吐方面显示出卓越的疗效，且不良反应很少，从而彻底改变了癌症患者的恶心治疗方法。本综述涵盖了作者在过去十年中在开发属于喹嗪相关芳基哌嗪衍生物类的 5-HT（3）R 配体方面所做的工作，这是对 2002 年在《当代药物化学》杂志上发表的综述的扩展。讨论主要集中在工作进展中出现的最重要的结构-亲和力关系上，并展示了原始想法在近年来是如何演变的。
