CP 945598 (Otenabant) is a potent and selective cannabinoid type 1 receptor antagonist that inhibits both basal and cannabinoid agonist-mediated CB(1) receptor signaling in vitro and in vivo. CP-945598 exhibits sub-nanomolar potency at human CB1 receptors in both binding (Ki = 0.7 nM) and functional assays (Ki = 0.2 nM) in vitro. CP-945598 (Otenabant) also acutely stimulates energy expenditure in rats and decreases the respiratory quotient indicating a metabolic switch to increased fat oxidation. A phase 1 study with CP-945598 of the roles of endocannabinoids in insulin secretion and action is recruiting.
|Animal models||Sprague-Dawley rats|
|Formulation||In 0.5% methyl cellulose|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Excretion, metabolism, and pharmacokinetics of CP-945,598, a selective cannabinoid receptor antagonist, in rats, mice, and dogs.
Miao Z, et al. Drug Metab Dispos. 2011 Dec;39(12):2191-208. PMID: 21875952.
In vitro and in vivo pharmacology of CP-945,598, a potent and selective cannabinoid CB(1) receptor antagonist for the management of obesity.
Hadcock JR, et al. Biochem Biophys Res Commun. 2010 Apr 2;394(2):366-71. PMID: 20211605.
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|WIN 55212-2 mesylate
WIN 55212-2 is a potent nanomolar affinity cannabinoid receptor agonist with Ki of 62.3 and 3.3 nM at the human cloned CB1 and CB2 receptors respectively.
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|CP 945598 hydrochloride
CP 945598 hydrochloride is a selective and high affinity CB1 antagonist (Ki values are 0.7 and 0.12 nM in binding and functional assays respectively).
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