Suvorexant (MK-4305) is a potent dual OX receptor antagonist with Ki of 0.55 nM and 0.35 nM for OX1 receptor and OX2 receptor, respectively. IC50 value: 0.55/0.35 nM(Ki, OX1/2) [1] Target:OX1R; OX2R in vivtro: in vivo: Suvorexant has excellent passive permeability and oral bioavailability, and induces favorable sleep effects in rats [1]. In addition, suvorexant significantly and dose-dependently reduces locomotor activity and promotes sleep in rats (10, 30, and 100 mg/kg), dogs (1 and 3 mg/kg), and rhesus monkeys (10 mg/kg) [2].
