Selective κ-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series

Andrew R. Jales, Stephen M. Husbands, John W. Lewis

Research output: Contribution to journalArticle

13 Citations (Scopus)


The study of κ-opioid receptor function in vivo has been hampered by the limited choice of selective κ-antagonists. Recently discovered κ-antagonists have not yet been utilised in vivo. We here report the synthesis and in vitro evaluation of a new amidine derivative of naltrindole. It showed substantially greater κ-selectivity in binding assays than known analogues with shorter spacer in the amidine side chain. This indicates that in nor-BNI and related selective κ-antagonists, the second basic centre may not be ideally located. (C) 2000 Elsevier Science Ltd.

Original languageEnglish
Pages (from-to)2259-2261
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Issue number20
Early online date9 Oct 2000
Publication statusPublished - 16 Oct 2000

ASJC Scopus subject areas

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

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