1-Substituted 4-(3-Hydroxyphenyl)piperazines Are Pure Opioid Receptor Antagonists
ACS Medicinal Chemistry Letters2010Vol. 1(7), pp. 365–369
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F. Ivy Carroll, Juan Pablo Cueva, James B. Thomas, S. Wayne Mascarella, Scott P. Runyon, Hernán A. Navarro
Abstract
This report describes the discovery that 1-substituted 4-(3-hydroxyphenyl)piperazines are pure opioid receptor antagonists. Compounds in this new series include N-phenylpropyl (3S)-3-methyl-4-(3-hydroxyphenyl)piperazine and (3R)-3-methyl-4-(3-hydroxyphenyl)piperazine, both of which diaplay low nanomolar potencies at μ, δ, and κ receptors and pure antagonist properties in a [(35)S]GTPγS assay.
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