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Description: Filorexant (formerly known as MK-6096) is a novel, orally bioavailable, potent and selective reversible antagonist of OX(1)R and OX(2)R currently in clinical development for insomnia. In radioligand binding and functional cell based assays, MK-6096 demonstrated potent binding and antagonism of both human OX(1)R and OX(2)R. MK-6096 occupies 90% of human OX(2)Rs expressed in transgenic rats at a plasma concentration of 142 nM, and dose-dependently reduced locomotor activity and significantly increased sleep in rats (3-30 mg/kg) and dogs (0.25 and 0.5 mg/kg). MK-6096 represents a novel and selective therapeutic for the treatment of insomnia.
References: Neuropharmacology. 2012 Feb; 62(2):978-87; ChemMedChem. 2012 Mar 5; 7(3):415-24, 337.
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