Cappelli Andrea, Anzini Maurizio, Vomero Salvatore, Mennuni Laura, Makovec Francesco, Hamon Michel, De Benedetti Pier G, Menziani M Cristina
Dipartimento Farmaco Chimico Tecnologico, Universit di Siena, Via A. Moro, 53100 Siena, Italy.
Curr Top Med Chem. 2002 Jun;2(6):599-624. doi: 10.2174/1568026023393813.
The serotonin 5-HT(3) receptor subtype is unique among the receptors for this neurotransmitter because it has been demonstrated to be a ligand-gated ion channel capable of mediating rapid intercellular communication. This review covers the authors work performed during more than a decade in the development of 5-HT(3) receptor ligands belonging to the classes of arylpiperazines, tropanes, and quinuclidine derivatives. The discussion is focused mainly on what the authors have learned about the interaction of these structurally different ligands with their receptor and shows the way their ideas evolved along with the progress of the project. Furthermore, a summary of the most significant structure-affinity relationships, derived from the original work, is reported to support the discussion.
血清素5-HT(3)受体亚型在该神经递质的受体中独具特色，因为它已被证实是一种能够介导快速细胞间通讯的配体门控离子通道。本综述涵盖了作者在十多年间开展的关于芳基哌嗪、托烷和奎宁环衍生物类5-HT(3)受体配体开发工作。讨论主要聚焦于作者对这些结构不同的配体与其受体相互作用的了解，并展示了他们的想法如何随着项目进展而演变。此外，还报告了源自原始工作的最重要的构效关系总结，以支持该讨论。
