Cinnamoyl Derivatives of 7α-Aminomethyl-6,14-endoethanotetrahydrothebaine and 7α-Aminomethyl-6,14-endoethanotetrahydrooripavine and Related Opioid Ligands

D Rennison, Adrian P Neal, Gerta Cami-Kobeci, Mario D Aceto, F Martinez-Bermejo, John W Lewis, S M Husbands

Research output: Contribution to journalArticle

13 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)5176-5182
Number of pages7
JournalJournal of Medicinal Chemistry
Volume50
Issue number21
DOIs
Publication statusPublished - 2007

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