trans-3,4-dimethyl-4-(3-carboxamidophenyl)piperidines: a novel class of micro-selective opioid antagonists.
Article Details
- CitationCopy to clipboard
Le Bourdonnec B, Belanger S, Cassel JA, Stabley GJ, DeHaven RN, Dolle RE
trans-3,4-dimethyl-4-(3-carboxamidophenyl)piperidines: a novel class of micro-selective opioid antagonists.
Bioorg Med Chem Lett. 2003 Dec 15;13(24):4459-62.
- PubMed ID
- 14643346 [ View in PubMed]
- Abstract
trans-3,4-Dimethyl-4-(3-carboxamidophenyl)piperidines constitute a novel class of micro opioid receptor antagonists. The CONH(2) group was found to be an effective isostere of the phenolic OH moiety. Structure-activity relationships at the piperidine nitrogen position led to the identification of several ligands displaying high affinity toward the cloned human micro opioid receptors, good selectivity micro/delta, micro/kappa, and potent in vitro antagonist activity.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Naloxone Kappa-type opioid receptor Ki (nM) 9.2 N/A N/A Details Naloxone Mu-type opioid receptor IC 50 (nM) 7.3 N/A N/A Details Naloxone Mu-type opioid receptor Ki (nM) 3.7 N/A N/A Details