AM251
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AM251
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| Systematic (IUPAC) name | |
| 1-(2,4-dichlorophenyl)-5-(4-iodophenyl]])-4-methyl- N-(1-piperidyl)pyrazole-3-carboxamide |
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| ATC code | ? |
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| Chemical data | |
| Formula | C22H21Cl2IN4O |
| Mol. mass | 555.238 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
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AM251 is a CB1 cannabinoid receptor antagonist. AM251 is structurally very close to SR141716A (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 SR141716A, which has a Ki value of 11.5 nM. However AM251 is about two-fold more selective for the CB1 receptor when compared to SR141716A.[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). PubMed: 10052983
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