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AM251



AM251
Systematic (IUPAC) name
1-(2,4-dichlorophenyl)-5-(4-iodophenyl]])-4-methyl-
N-(1-piperidyl)pyrazole-3-carboxamide
Identifiers
CAS number  ?
ATC code  ?
PubChem 2125
Chemical data
Formula C22H21Cl2IN4O 
Mol. mass 555.238 g/mol
Pharmacokinetic data
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Therapeutic considerations
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Legal status
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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]

Additional recommended knowledge


References

  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



 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "AM251". A list of authors is available in Wikipedia.
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