Description
Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist ( pK i values of 8.0 and 8.1 for human and rat OX2R). Seltorexant hydrochloride crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brainIn VivoSeltorexant hydrochloride (JNJ-42847922 hydrochloride) (3-30 mg/kg; p.o.) dose-dependently induces and prolongs sleep in male Sprague-Dawley rats. The sleep-promoting effects of Seltorexant hydrochloride (30 mg/kg; p.o.; per day for 7 days) are maintained upon 7-day repeated dosing in rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague-Dawley rats (350-450 g) Dosage: 30 mg/kg Administration: p.o.; per day for 7 days Result: The reduced sleep onset (non–rapid eye movement (NREM) latency) and the increased NREM sleep duration were maintained upon 7-day repeated dosing with JNJ-42847922. The prolongation of NREM sleep time was due to a significant increase in NREM bout duration throughout the treatment period assessed on D1 and D7. Rapid eye movement (REM) sleep was only marginally affected on D4 of treatment, resulting in a small but significant reduction in REM sleep latency and an increase in REM sleep duration.IC50& Target:human OX2R 8.0 (pKi) rat OX2R 8.1 (pKi)