AM251

AM251
Systematic (IUPAC) name
	1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-; N-(1-piperidyl)pyrazole-3-carboxamide
Clinical data
Pregnancy cat.	?
Legal status	?
Identifiers
CAS number	183232-66-8
ATC code	?
PubChem	CID 2125
IUPHAR ligand	744
ChemSpider	2040
ChEMBL	CHEMBL285932
Chemical data
Formula	C22H21Cl2IN4O
Mol. mass	555.238 g/mol
SMILES	eMolecules & PubChem
	InChI InChI=1S/C22H21Cl2IN4O/c1-14-20(22(30)27-28-11-3-2-4-12-28)26-29(19-10-7-16(23)13-18(19)24)21(14)15-5-8-17(25)9-6-15/h5-10,13H,2-4,11-12H2,1H3,(H,27,30) ; Key:BUZAJRPLUGXRAB-UHFFFAOYSA-N ;
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AM-251 is an inverse agonist at the CB₁ cannabinoid receptor. AM-251 is structurally very close to SR141716A (rimonabant), which both are biarylpyrazole cannabinoid receptor antagonists. In AM-251 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 K_i value of 7.5nM) than SR141716A, which has a K_i value of 11.5nM, AM-251 is, however, about two-fold more selective for the CB₁ receptor when compared to SR141716A.^[1]

[edit] See also

^ 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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