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.
Neurobiol Aging. 2020 Jul;91:66-75.
Suvorexant ameliorates cognitive impairments and pathology in APP/PS1 transgenic mice
Suvorexant purchased from AbMole
|Source||Neurobiology of Aging 2020 Jul. Figure 1. Suvorexant (Abmole Bioscience, USA)|
|Cell Lines||AD model mice|
|Incubation Time||4 weeks|
|Results||However, compared with 61.8% 2.6% in WT-Veh group, the percentage of correct spontaneous alternation of APP/PS1-Veh group significantly decreased to 48.6% 3.6% (p¼0.001), while suvorexant treatment increased the percentage of APP/PS1 mice to 70.6% 2.4%|
|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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
|Solubility||DMSO 10 mg/mL|
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|
OXA (17-33) is a potent and selective peptide orexin OX1 receptor agonist (EC50 values are 8.29 and 187 nM for OX1 and OX2 receptors respectively).
|Orexin 2 Receptor Agonist
Orexin 2 Receptor Agonist (ABM-565520) is a potent and selective Orexin2 receptor agonist with EC50 value of 23 nM.
Lemborexant (E-2006) is an orally active, competitive and reversible dual OX1 and OX2 receptors antagonist, with IC50 values of 6.1 nM and 2.6 nM, respectively.
|Orexin A (human, mouse, rat, bovine)
Orexin A (human, mouse, rat, bovine) is a specific, high-affinity agonist for G-protein-coupled receptor OX1R.
MK-1064 is a potent, selective and orally active Orexin OX2 Receptor Antagonist for the research of insomnia.
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