2. Academic Validation
  3. 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. [email protected]
PMID: 18313920 DOI: 10.1016/j.bmcl.2008.01.106
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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