1. Academic Validation
  2. Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as mu opioid receptor antagonists with improved opioid receptor selectivity profiles

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

  • Bioorg Med Chem Lett. 2008 Mar 15;18(6):2006-12. doi: 10.1016/j.bmcl.2008.01.106.
Bertrand Le Bourdonnec 1 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
Affiliations

Affiliation

  • 1 Department of Chemistry, Adolor Corporation, 700 Pennsylvania Drive, Exton, PA 19341, USA. blebourdonnec@adolor.com
Abstract

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

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