Discovery of the First N-Substituted 4β-Methyl-5-(3-hydroxyphenyl)morphan To Possess Highly Potent and Selective Opioid δ Receptor Antagonist Activity

A structurally novel opioid δ receptor selective antagonist has been identified. This compound, (+)-5-(3-hydroxyphenyl)-4-methyl-2-(3-phenylpropyl)-2-azabicyclo[3.3.1]non-7-yl-(1-phenyl-1-cyclopentane)carboxamide [(+)-KF4, (+)-4], showed a K e value of 0.15 nM in the [35S]GTPγS functional assay. (+)...

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Veröffentlicht in:Journal of medicinal chemistry 2004-01, Vol.47 (2), p.281-284
Hauptverfasser: Carroll, F. Ivy, Zhang, Li, Mascarella, S. Wayne, Navarro, Hernán A, Rothman, Richard B, Cantrell, Buddy E, Zimmerman, Dennis M, Thomas, James B
Format: Artikel
Sprache:eng
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