Cinnamoyl derivatives of 7α-aminomethyl-6,14-endo- ethanotetrahydrothebaine and 7α-aminomethyl-6,14-endo- ethanotetrahydrooripavine and related opioid ligands

David Rennison, Adrian P. Neal, Gerta Cami-Kobeci, Mario D. Aceto, Fernando Martinez-Bermejo, John W. Lewis, Stephen M. Husbands

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    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
    Early online date22 Sept 2007
    DOIs
    Publication statusPublished - 18 Oct 2007

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