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

[摘要]：This report describes the discovery that 1-substituted 4-(3-hydroxy-phenyl)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 display low nanomolar potencies at mu, delta and kappa receptors and pure antagonist properties in a[S-35]GTP gamma S assay.

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