Synthesis and binding properties of novel selective 5-HT3 receptor ligands

Maria Modica, Giuseppe Romeo, Luisa Materia, Filippo Russo, Alfredo Cagnotto, Tiziana Mennini, Róbert Gáspár, George Falkay, Ferenc Fülöp

Research output: Article

35 Citations (Scopus)


This work reports on the synthesis and affinities for the 5-HT3 versus the 5-HT4 receptor of new piperazinyl-substituted thienopyrimidine derivatives 20-45 with a view to identify potent and selective ligands for the 5-HT3 receptor. Some of the new compounds show good affinity for the 5-HT3 receptor and, notably, do not display any affinity for the 5-HT4 receptor. 4-(4-Methyl-1-piperazinyl)-2- methylthio-6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidine 31 exhibits the highest affinity for the 5-HT3 receptor (Ki=33nM) and behaves as noncompetitive antagonist.

Original languageEnglish
Pages (from-to)3891-3901
Number of pages11
JournalBioorganic and Medicinal Chemistry
Issue number14
Publication statusPublished - júl. 15 2004


ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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