Pyrrolo- and pyridomorphinans: Non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists

V. Kumar, M.J. Clark, J.R. Traynor, J.W. Lewis, S.M. Husbands

Research output: Contribution to journalArticle

2 Citations (Scopus)
61 Downloads (Pure)

Abstract

Opioid ligands have found use in a number of therapeutic areas, including for the treatment of pain and opiate addiction (using agonists) and alcohol addiction (using antagonists such as naltrexone and nalmefene). The reaction of imines, derived from the opioid ligands oxymorphone and naltrexone, with Michael acceptors leads to pyridomorphinans with structures similar to known pyrrolo- and indolomorphinans. One of the synthesized compounds, 5e, derived from oxymorphone had substantial agonist activity at delta opioid receptors but not at mu and/or kappa opioid receptors and in that sense profiled as a selective delta opioid receptor agonist. The pyridomorphinans derived from naltrexone and naloxone were all found to be non-selective potent antagonists and as such could have utility as treatments for alcohol abuse.

Original languageEnglish
Pages (from-to)4067-4072
JournalBioorganic and Medicinal Chemistry
Volume22
Issue number15
Early online date12 Jun 2014
DOIs
Publication statusPublished - 1 Aug 2014

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