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8-(Heteroaryl)phenalkyl-1-Phenyl-1,3,8-triazaspiro[4.5]decan-4-ones as Opioid Receptor Modulators

[ Vol. 1 , Issue. 6 ]

Author(s):

A. D. Jordan, M. J. Orsini, S. A. Middleton, P. J. Connolly, D. E. Brenneman, K. Pan and A. B. Reitz   Pages 601 - 610 ( 10 )

Abstract:


A series of N-biarylalkyl-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-ones were prepared and evaluated for biological activity at opioid (μ, δ, κ) and opioid receptor like-1 (ORL-1) G-protein coupled receptors. Substitution on the biaryl moiety produced enhanced affinity for the μ-opioid receptor.

Keywords:

mu receptor, delta receptor, kappa receptor, nociceptin receptor, pain, 1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one, heteroarylphenylalkyl, sar, [35s]gtpγs binding assay, suzuki reaction

Affiliation:

Drug Discovery Division, Johnson&Johnson Pharmaceutical Research and Development, LLC, aP.O. Box 776, Welsh and McKean Rds., Spring House, PA 19477-0777, USA.



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