Seltorexanthydrochloride(JNJ-42847922hydrochloride)是一种具有口服活性的，高亲和性以及选择性的OX2R拮抗剂(人和大鼠中的OX2R的pKi值分别为8.0和8.1)。Seltorexanthydrochloride穿过血脑屏障，迅速占据大鼠大脑中的OX2R结合位点。
Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist (pKi 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 brain[1].
Seltorexant hydrochloride (JNJ-42847922 hydrochloride) (3-30 mg/kg; p.o.) dose-dependently induces and prolongs sleep in male Sprague-Dawley rats[1].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[1]. Animal Model: Male Sprague-Dawley rats (350-450 g)[1]
[1]. Bonaventure P, et al. Characterization of JNJ-42847922, a Selective Orexin-2 Receptor Antagonist, as a Clinical Candidate for the Treatment of Insomnia. J Pharmacol Exp Ther. 2015 Sep;354(3):471-82.
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