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1-Substituted 4-(3-Hydroxyphenyl)piperazines Are Pure Opioid Receptor Antagonists.
- Source :
-
ACS medicinal chemistry letters [ACS Med Chem Lett] 2010 Oct 14; Vol. 1 (7), pp. 365-369. - Publication Year :
- 2010
-
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.
Details
- Language :
- English
- ISSN :
- 1948-5875
- Volume :
- 1
- Issue :
- 7
- Database :
- MEDLINE
- Journal :
- ACS medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 21116435
- Full Text :
- https://doi.org/10.1021/ml100126b