My watch list
my.chemeurope.com  

my.chemeurope.com

With an accout for my.chemeurope.com you can always see everything at a glance – and you can configure your own website and individual newsletter.

  • My watch list
  • My saved searches
  • My saved topics
  • My newsletter
Register free of charge
Login  
eng  
DeutschEnglishFrançaisEspañol

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
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?

Legal status
Routes  ?

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

  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



v • d • e
Cannabinoids
Plant cannabinoidsCBD • CBDV • CBN • CBG • CBV • CBL • THC • THC-C4 • 11-Hydroxy-THC • THCV
Synthetic cannabinoidsAjulemic acid • AM251 • CP 55,940 • DMHP • Dronabinol • HU-210 • JWH-133 • Levonantradol • Methanandamide • Nabilone • Nabitan • Parahexyl • Pravadoline • Rimonabant • THC-O-acetate • THC-O-phosphate • WIN 55,212-2
Endogenous cannabinoidsArachidonoyl ethanolamide (Anandamide or AEA) • 2-Arachidonoylglycerol (2-AG) • 2-Arachidonyl glyceryl ether (noladin ether) • Virodhamine • N-arachidonoyl-dopamine (NADA)
 
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.
Your browser is not current. Microsoft Internet Explorer 6.0 does not support some functions on Chemie.DE