University of Hertfordshire

  • David Rennison
  • Adrian P. Neal
  • Gerta Cami-Kobeci
  • Mario D. Aceto
  • Fernando Martinez-Bermejo
  • John W. Lewis
  • Stephen M. Husbands
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Original languageEnglish
Number of pages7
Pages (from-to)5176-5182
JournalJournal of Medicinal Chemistry
Journal publication date18 Oct 2007
Volume50
Issue21
Early online date22 Sep 2007
DOIs
Publication statusPublished - 18 Oct 2007

Abstract

A new series of ligands has been synthesized where the cinnamoyl group of the 14-cinnamoylamino morphinones has been introduced to the 7α-substituent of the 6,14-bridged oripavine series. In vitro the compounds were mostly low efficacy partial agonists or antagonists with some selectivity for the mu opioid receptor, with evidence of mu efficacy in vivo. The similarity in SAR between these 6,14-bridged oripavines and the 14-cinnamoylamino series suggests a similar mode of interaction with the mu opioid receptor.

Notes

© 2007 American Chemical Society.

ID: 16762253