AM251
From Wikipedia, the free encyclopedia
| AM251 | |
 |
|
| Chemical formula | C22H21N4ICl2O |
| Molar mass | 555.238 g mol−1 |
| Systematic name | 1-(2,4-dichlorophenyl)-5-(4-iodophenyl]])-4-methyl-N-(1-piperidyl)pyrazole-3-carboxamide |
| Complete data | |
AM251 is a CB1 cannabinoid receptor antagonist. AM251 is structurally very close to SR 141716A (rimonabant), which both are biarylpyrazole cannabinoid receptor antagonists. In AM251 the p-chloro group attached to the phenyl substituent at C-5 of the pyrazole ring is replaced with a p-iodo group. The resulting compound exhibits slightly better binding affinity for the CB1 receptor with a Ki value of 7.5 nM compound to SR 141716A, which has a Ki value of 11.5 nM. However AM251 is about two-fold more selective for the CB1 receptor when compared to SR 141716A.[1]
[edit] References
- Lan, R., Liu, Q., Fan, P., et al. Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists. J Med Chem 42 769-776 (1999).
 |
This pharmacology-related article is a stub. You can help Wikipedia by expanding it. |
Anandamide • 2-AG • CBD • CBDV • CBN • CBV • CP 55,940 • HU-210 • Levonantradol • JWH-133 • Nabilone • THC • THCV • URB597 • URB754 • WIN 55,212-2 • Rimonabant • AM251 • THC-O-phosphate • Parahexyl
