Seltorexant (JNJ-42847922) is an orally active, high-affinity, and selective orexin-2 receptor (OX2R) antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain.IC50 & Target: pKi: 8.0 (human OX2R), 8.1 (rat OX2R)In Vivo: Seltorexant (JNJ-42847922) (3-30 mg/kg; p.o.) dose-dependently induces and prolongs sleep in male Sprague-Dawley rats.
The sleep-promoting effects of JNJ-42847922 (30 mg/kg; p.o.; per day for 7 days) are maintained upon 7-day repeated dosing in rats.