The Interactions of the 5-HT3 Receptor with Quipazine-Like Arylpiperazine Ligands. The Journey Track at the End of the First Decade of the Third Millennium

Title: The Interactions of the 5-HT3 Receptor with Quipazine-Like Arylpiperazine Ligands. The Journey Track at the End of the First Decade of the Third Millennium

Volume: 10 Issue: 5

Author(s): Andrea Cappelli, Stefania Butini, Antonella Brizzi, Sandra Gemma, Salvatore Valenti, Germano Giuliani, Maurizio Anzini, Laura Mennuni, Giuseppe Campiani, Vittorio Brizzi and Salvatore Vomero

Affiliation:

Abstract: The 5-HT3 receptor (5-HT3R) 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-HT3R 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-HT3R 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 mainly focused 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.

Cite this article as:

Cappelli Andrea, Butini Stefania, Brizzi Antonella, Gemma Sandra, Valenti Salvatore, Giuliani Germano, Anzini Maurizio, Mennuni Laura, Campiani Giuseppe, Brizzi Vittorio and Vomero Salvatore, The Interactions of the 5-HT3 Receptor with Quipazine-Like Arylpiperazine Ligands. The Journey Track at the End of the First Decade of the Third Millennium, Current Topics in Medicinal Chemistry 2010; 10 (5) . https://dx.doi.org/10.2174/156802610791111560