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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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Publication details

The article was received on 07 Dec 2010, accepted on 17 Feb 2011 and first published on 09 Mar 2011


Article type: Concise Article
DOI: 10.1039/C0MD00249F
Med. Chem. Commun., 2011,2, 413-417

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    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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