Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as μ opioid receptor antagonists with improved opioid receptor selectivity profiles

Bertrand Le Bourdonnec, William M. Barker, Serge Belanger, Daniel D. Wiant, Nathalie C. Conway-James, Joel A. Cassel, Timothy J. O'Neill, Patrick J. Little, Robert N. DeHaven, Diane L. DeHaven-Hudkins, Roland E. Dolle

Research output: Contribution to journalArticlepeer-review

5 Scopus citations

Abstract

A series of N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines, μ opioid receptor antagonists, analogs of alvimopan, were prepared using solid phase methodology. This study led to the identification of a highly selective μ opioid receptor antagonist, which interacts selectively with μ peripheral receptors.

Original languageEnglish
Pages (from-to)2006-2012
Number of pages7
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number6
DOIs
StatePublished - Mar 15 2008

Keywords

  • Opioid
  • Solid phase synthesis
  • μ receptors

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