Otenabant (CP-945598) HCl 686347-12-6

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Molecular Weight:

546.88 Otenabant (CP-945598) HCl 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. Phase 1.

Biological Activity

CP-945598 HCl inhibits CB1 receptor with moderate unbound microsomal clearance, low hERG affinity, and adequate CNS penetration. CP-945598 HCl has low affinity with Ki of 7.6 μM for human CB2 receptors.


CP-945598 HCl reverses four cannabinoid agonistmediated behaviors
(locomotor activity, hypothermia, analgesia, and catalepsy) following
administration of the synthetic CB1 receptor agonist
CP-55940.


CP-945598 HCl exhibits dose-dependent anorectic activity in a
model of acute food intake in rodents and increased energy expenditure
and fat oxidation. CP-945598 also acutely stimulates
energy expenditure in rats and decreases the respiratory quotient
indicating a metabolic switch to increased fat oxidation. CP-945598 at
10 mg/kg promotes a 9%, vehicle adjusted weight loss in a 10 day weight
loss study in diet-induced obese mice.

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Product Categories : GPCR & G Protein > Cannabinoid Receptor Inhibitor