Rimonabant

Rimonabant is a cannabinoid 1 (CB1) receptor antagonist (Ki = 5.6 nM). It is selective for CB1 over CB2 receptors (Ki = >1,000 nM), as well as a panel of 37 other receptors and channels (IC50s = >1,000 nM). Rimonabant (10 µM) inhibits phytohemagglutinin-induced proliferation of isolated human peripheral blood mononuclear cells (PBMCs). Intraperitoneal administration of rimonabant prevents decreases in body temperature and increases in tail-flick latency induced by the CB1 and CB2 receptor agonist (+)-WIN 55,212-2 (Cay-10009023) in mice (ED50s = 0.28 and 1.62 mg/kg, respectively) and oral administration reduces body weight in a mouse model of diet-induced obesity when administered at a dose of 10 mg/kg in the drinking water. Rimonabant (10 mg/kg) decreases the percentage of time spent in the open arms of the elevated plus maze in mice, indicating anxiety-like activity. Formulations containing rimonabant have previously been used in the treatment of obesity.Formal Name: 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-1-piperidinyl-1H-pyrazole-3-carboxamide. CAS Number: 168273-06-1. Synonyms: SR141716. Molecular Formula: C22H21Cl3N4O. Formula Weight: 463.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS (pH 7.2)(1:2): 0.3 mg/ml. SMILES: Clc1ccc(cc1)c1c(C)c(nn1c1ccc(Cl)cc1Cl)C(=O)NN1CCCCC1. InChi Code: InChI=1S/C22H21Cl3N4O/c1-14-20(22(30)27-28-11-3-2-4-12-28)26-29(19-10-9-17(24)13-18(19)25)21(14)15-5-7-16(23)8-6-15/h5-10,13H,2-4,11-12H2,1H3,(H,27,30). InChi Key: JZCPYUJPEARBJL-UHFFFAOYSA-N.