Suvorexant (MK-4305) is a dual orexin receptor antagonist currently under clinical investigation as a novel therapy for insomnia. Suvorexant is not currently approved for commercial use, but it has completed three Phase III trials. The recent FDA review showed that Suvorexant (MK-4305) is associated with increased somnolence the next day and users of higher doses had an increased rate of suicidal ideation. Suvorexant works by turning off wakefulness rather than by inducing sleep.
|Animal models||human OX 2 R expressed in transgenic rats|
|Formulation||25% hydroxypropyl- β -cyclodextrin|
|Dosages||0.1 – 2.0 mg/ kg|
|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.
Promotion of sleep by suvorexant-a novel dual orexin receptor antagonist.
Winrow CJ, et al. J Neurogenet. 2011 Mar;25(1-2):52-61. PMID: 21473737.
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MK-3697 is an isonicotinamide small molecule, acting as a potent and selective Orexin 2 receptor antagonist with Ki = 0.95 nM.
SB408124 (Tocris-1963) is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and27 nM in both whole cell and membrane, respectively, exhibits 50-fold selectivity over OX2 receptor.
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