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Medicinal Chemistry

Author(s): A. D. Jordan, M. J. Orsini, S. A. Middleton, P. J. Connolly, D. E. Brenneman, K. Pan and A. B. Reitz

DOI: 10.2174/157340605774598207

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

Page: [601 - 610] Pages: 10

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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