Issue 10, 2011

Discovery of CP-866,087, a mu opioid receptor antagonist for the treatment of alcohol abuse and dependence

Abstract

CP-866,087 (compound 15) is a novel, potent and selective mu opioid receptor antagonist. The design rationale, synthesis, in vitro and in vivo biological evaluation are reported herein. Preclinical efficacy data in disease relevant models measuring reduction of alcohol intake are presented, along with preclinical pharmacokinetic properties which supported the selection of the title compound for clinical evaluation.

Graphical abstract: Discovery of CP-866,087, a mu opioid receptor antagonist for the treatment of alcohol abuse and dependence

Supplementary files

Article information

Article type
Concise Article
Submitted
23 Jun 2011
Accepted
27 Jul 2011
First published
25 Aug 2011

Med. Chem. Commun., 2011,2, 1001-1005

Discovery of CP-866,087, a mu opioid receptor antagonist for the treatment of alcohol abuse and dependence

S. F. McHardy, S. D. Heck, S. Guediche, M. Kalman, M. P. Allen, M. Tu, D. K. Bryce, A. W. Schmidt, M. Vanase-Frawley, E. Callegari, S. Doran, N. J. Grahame, S. McLean and S. Liras, Med. Chem. Commun., 2011, 2, 1001 DOI: 10.1039/C1MD00164G

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