University of Hertfordshire

Mixed k/μ opioid receptor agonists: The 6β-naltrexamines

Research output: Contribution to journalArticlepeer-review

  • Gerta Cami-Kobeci
  • Adrian P. Neal
  • Faye A. Bradbury
  • Lauren C. Purington
  • Mario D. Aceto
  • Louis S. Harris
  • John W. Lewis
  • John R. Traynor
  • Stephen M. Husbands
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Original languageEnglish
Pages (from-to)1546-1552
Number of pages7
JournalJournal of Medicinal Chemistry
Volume52
Issue6
Early online date2 Mar 2009
DOIs
Publication statusPublished - 26 Mar 2009

Abstract

Ligands from the naltrexamine series have consistently demonstrated agonist activity at κ opioid receptors (KOR), with varying activity at the μ opioid receptor (MOR). Various 6β-cinnamoylamino derivatives were made with the aim of generating ligands with a KOR agonist/MOR partial agonist profile, as ligands with this activity may be of interest as treatment agents for cocaine abuse. The ligands all displayed the desired high affinity, nonselective binding in vitro and in the functional assays were high efficacy KOR agonists with some partial agonist activity at MOR. Two of the new ligands (12a, 12b) have been evaluated in vivo, with 12a acting as a KOR agonist and therefore somewhat similar to the previously evaluated analogues 3-6, while 12b displayed predominant MOR agonist activity.

Notes

© 2009 American Chemical Society

ID: 16762136