Novel, potent, and selective quinoxaline-based 5-HT3 receptor ligands. 1. Further structure-activity relationships and pharmacological characterization

Stefania Butini, Roberta Budriesi, Michel Hamon, Elena Morelli, Sandra Gemma, Margherita Brindisi, Giuseppe Borrelli, Ettore Novellino, Isabella Fiorini, Pierfranco Ioan, Alberto Chiarini, Alfredo Cagnotto, Tiziana Mennini, Claudia Fracasso, Silvio Caccia, Giuseppe Campiani

Research output: Contribution to journalArticlepeer-review

Abstract

We investigated the pharmacological profile of a novel series of quinoxaline-based 5-HT3 receptor ligands bearing an extra basic moiety on the piperazine N-4. High affinity and selectivity were dependent on the electronic properties of the substituents, and at cardiac level 3a and 3c modulated chronotropy but not inotropy. In von Bezold-Jarisch reflex test 3a-c were partial agonists while 3i was a full agonist. Preliminary pharmacokinetic studies indicated that 3a is a brain penetrating agent.

Original languageEnglish
Pages (from-to)6946-6950
Number of pages5
JournalJournal of Medicinal Chemistry
Volume52
Issue number21
DOIs
Publication statusPublished - Nov 12 2009

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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