6N-cinnamoyl-β-naltrexamine and its p-nitro derivative. High efficacy κ-opioid agonists with weak antagonist actions

Ian Derrick, Humphrey A. Moynihan, Jillian Broadbear, James H. Woods, John W. Lewis

Research output: Contribution to journalArticle

12 Scopus citations

Abstract

6N-cinnamoyl-β-naltrexamine and its p-nitro derivative (7 and 8) are κ-opioid agonists of high potency and exceptional efficacy and are only weakly effective μ opioid antagonists. This contrasts with the p-methyl analogue which has only low efficacy κ-agonism but is a selective irreversible μ-antagonist like β-FNA.

Original languageEnglish (US)
Pages (from-to)167-172
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume6
Issue number2
DOIs
StatePublished - Jan 23 1996
Externally publishedYes

ASJC Scopus subject areas

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

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