| Identification | Back Directory | [Name]
Otenabant | [CAS]
686344-29-6 | [Synonyms]
CS-1072
otenabant
Otenabant, >=98%
CP945598 free base
Otenabant (CP-945,598)
CP 945598;OTENABANT;CP945598
CP 945598; CP-945598; CP945598
Otenabant (CP-945598 free base)
1-[9-(4-Chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxamide
4-Piperidinecarboxamide, 1-[8-(2-chlorophenyl)-9-(4-chlorophenyl)-9H-purin-6-yl]-4-(ethylamino)- | [Molecular Formula]
C25H25Cl2N7O | [MOL File]
686344-29-6.mol | [Molecular Weight]
510.42 |
| Chemical Properties | Back Directory | [Boiling point ]
757.9±70.0 °C(Predicted) | [density ]
1.46 | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (195.92 mM; Need ultrasonic) | [form ]
Powder | [pka]
16.30±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Otenabant is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor. | [Biological Activity]
Otenabant is a potent and selective cannabinoid receptor CB1 antagonist with a Ki of 0.7 nM, more than 1000-fold selective for CB2. | [in vitro]
Otenabant HCl has low affinity with K i of 7.6 μM for human CB2 receptors. It inhibits CB1 receptor with moderate unbound microsomal clearance, low hERG affinity, and adequate CNS penetration. < /p> | [in vivo]
Otenabant acutely stimulates energy expenditure in rats and decreases the respiratory quotient indicating a metabolic switch to increased fat oxidation. It (10 mg/kg, po) promotes a 9%, vehicle adjusted weight loss in a 10 day weight loss study in diet-induced obese mice. Otenabant HCl reverses four cannabinoid agonistmediated behaviors (locomotor activity, hypothermia, analgesia, and catalepsy) following administration of the synthetic CB1 receptor agonist CP-55940. And Otenabant HCl exhibits dose-dependent anorectic activity in a model of acute food intake in rodents and increased energy expenditure and fat oxidation. | [target]
| [References]
[1] John R. Hadcock, et al. In vitro and in vivo pharmacology of CP-945,598, a potent and selective cannabinoid CB1 receptor antagonist for the management of obesity. Biochemical and Biophysical Research Communications, 2010; 394;366-371.
[2] Griffith DA, et al. Discovery of 1-[9-(4-chlorophenyl) -8-(2-chlorophenyl)- 9H-purin-6-yl] -4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist. JMedChem. 2009 ;5 |
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