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Bioorg Med Chem Lett. 2006 Jan 1;16(1):146-9. Epub 2005 Oct 19.

4-Phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives, a novel class of selective delta-opioid agonists.

Author information

1
Division of Psychiatry, Research and Early Development Europe, Johnson and Johnson Pharmaceutical Research and Development, Jarama 75, 47007 Toledo, Spain. atrabanc@prdes.jnj.com

Abstract

A novel series of 4-phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives has been prepared and their synthesis described herein. In vitro affinities for delta-, mu-, and kappa-opioid receptors, as well as the functional activity in the [(35)S]GTPgammaS assay are reported. The most potent and selective delta-opioid agonist 18a exhibited a K(i) of 18 nM, and was >258-fold and 28-fold selective over mu- and kappa-receptors, respectively; the compound is a full agonist with an EC(50) value of 14 nM.

PMID:
16236510
DOI:
10.1016/j.bmcl.2005.09.025
[Indexed for MEDLINE]

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