AM251

AM251
	File:AM2512d.png
	File:AM2513d.png
Identifiers
	IUPAC name 1-(2,4-dichlorophenyl)-5-(4-iodophenyl]])-4-methyl-; N-(1-piperidyl)pyrazole-3-carboxamide;
PubChem CID	2125;
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
Formula	C22H21Cl2IN4O
Molar mass	555.238 g/mol

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]

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). Template:PubMed

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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). Template:PubMed

[1]

Identifiers
File:AM2512d.png
File:AM2513d.png
IUPAC name 1-(2,4-dichlorophenyl)-5-(4-iodophenyl]])-4-methyl- N-(1-piperidyl)pyrazole-3-carboxamide
PubChem CID	2125
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
Formula	C₂₂H₂₁Cl₂IN₄O
Molar mass	555.238 g/mol

AM251

References

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