• Journal Article

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

Citation

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. DOI: 10.1021/ml100126b

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