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1-Substituted 4-(3-Hydroxyphenyl)piperazines Are Pure Opioid Receptor Antagonists.

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.

SUBMITTER: Carroll FI

PROVIDER: S-EPMC2992360 | biostudies-literature | 2010 Oct

REPOSITORIES: biostudies-literature

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1-Substituted 4-(3-Hydroxyphenyl)piperazines Are Pure Opioid Receptor Antagonists.

Carroll F Ivy FI Cueva Juan Pablo JP Thomas James B JB Mascarella S Wayne SW Runyon Scott P SP Navarro Hernán A HA

ACS medicinal chemistry letters 20101001 7

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. ...[more]

PMID: 21116435

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2024-06-01 | GSE266932 | GEO

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