High potent and selective arylpiperazine derivatives as ligands for the 5-HT(1A) receptor

Maria Modica, Maria Santagati, Andrea Santagati, Filippo Russo, Alfredo Cagnotto, Mara Goegan, Tiziana Mennini

Research output: Contribution to journalArticlepeer-review

Abstract

This paper reports the synthesis and affinities on the 5-HT(1A) versus the α1A receptors of new arylpiperazinylalkylthiothienopyrimidine and thiadiazole derivatives 16-24. Arylpiperazines 16-23 show affinities values in the nanomolar range for the 5-HT(1A) receptor. The compound 16 is highly potent (K(i) 0.26 nM, selectivity 28), the derivatives 20 and 21 are less potent, but highly selective (K(i) 9.40 and 5.06 nM, selectivity 207 and 73, respectively). (C) 2000 Elsevier Science Ltd. All rights reserved.

Original languageEnglish
Pages (from-to)1089-1092
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume10
Issue number10
DOIs
Publication statusPublished - May 15 2000

ASJC Scopus subject areas

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

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