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Issue 5, 2011
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Discovery and pharmacological characterization of a selective delta opiate receptor antagonist (CP-646,777)

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Abstract

CP-646,777 (compound 2a) is identified as a potent and selective delta opioid receptor antagonist. The synthesis, pharmacological evaluation, disposition characteristics and pharmacokinetic properties of this compound are reported herein. An approach for reducing clearance as measured by human liver microsomes is demonstrated. The significance of p-glycoprotein efflux on CNS disposition and on the pharmacological action of CP-646,777 is also discussed.

Graphical abstract: Discovery and pharmacological characterization of a selective delta opiate receptor antagonist (CP-646,777)

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Article information


Submitted
07 Dec 2010
Accepted
17 Feb 2011
First published
09 Mar 2011

Med. Chem. Commun., 2011,2, 413-417
Article type
Concise Article

Discovery and pharmacological characterization of a selective delta opiate receptor antagonist (CP-646,777)

S. Liras, S. F. McHardy, M. P. Allen, B. E. Segelstein, S. D. Heck, D. K. Bryce, A. W. Schmidt, R. O'Connor, M. Vanase-Frawley, E. Callegari and S. McLean, Med. Chem. Commun., 2011, 2, 413
DOI: 10.1039/C0MD00249F

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