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Bioorg Med Chem Lett. 2005 May 16;15(10):2647-52.

Arylacetamide kappa opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity.

Author information

1
Department of Chemistry, Adolor Corporation, 700 Pennsylvania Drive, Exton, PA 19341, USA. blebourdonnec@adolor.com

Abstract

Some kappa opioid receptor agonists of the arylacetamide class, for example, ICI 199441 (1), were found to strongly inhibit the activity of cytochrome P450 2D6 (CYP2D6) (1: CYP2D6 IC50=26 nM). Certain analogs bearing a substituted sulfonylamino group, for example, 13, were discovered to have significantly reduced CYP2D6 inhibitory activity (13: CYP2D6 IC50>10 microM) while displaying high affinity toward the cloned human kappa opioid receptor, good kappa/delta and kappa/mu selectivity, and potent in vitro and in vivo agonist activity.

PMID:
15863335
DOI:
10.1016/j.bmcl.2005.03.020
[Indexed for MEDLINE]

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