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.
|Related OX Receptor Products|
MK-1064 is a potent, selective and orally active Orexin OX2 Receptor Antagonist for the research of insomnia.
SB-649868 is a selective orally active orexin (OX) receptor antagonist with pKi values of 9.4 and 9.5 at the OX1 and OX2 receptor, respectively.
SB-334867 is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2.
TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively).
MK-3697 is an isonicotinamide small molecule, acting as a potent and selective Orexin 2 receptor antagonist with Ki = 0.95 nM.
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