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

F. Ivy Carroll; S. Mascarella; Hernan A. Navarro; James B. Thomas; Scott P. Runyon; Ivy Carroll; Juan Cueva; James B. Thomas; S. Wayne Mascarella; Scott P. Runyon; Hernan A. Navarro

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

Carroll, F., Cueva, J., Thomas, J., Mascarella, S., Runyon, S., & Navarro, H. (2010). 1-Substituted 4-(3-Hydroxyphenyl)piperazines Are Pure Opioid Receptor Antagonists. ACS Medicinal Chemistry Letters, 1(7), 365-369. https://doi.org/10.1021/ml100126b

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Abstract

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