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

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.

journal_name

Bioorg Med Chem Lett

authors

Le Bourdonnec B,Barker WM,Belanger S,Wiant DD,Conway-James NC,Cassel JA,O'Neill TJ,Little PJ,DeHaven RN,DeHaven-Hudkins DL,Dolle RE

doi

10.1016/j.bmcl.2008.01.106

subject

Has Abstract

pub_date

2008-03-15 00:00:00

pages

2006-12

issue

6

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(08)00133-9

journal_volume

18

pub_type

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