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
Identifiers
CAS Number 183232-66-8
PubChem CID 2125
IUPHAR/BPS 744
Chemical data
Formula C22H21Cl2IN4O
Molar mass 555.238 g/mol[[Script error: No such module "String".]]
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AM251 is an inverse agonist at the CB1 cannabinoid receptor. 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]

See also

References

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  1. ↑ 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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