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Seltorexant, also known as JNJ-42847922 and MIN-202, is a potent OX2R antagonist that has been shown to promote sleep in various species. JNJ-42847922 had an approximate 2-log selectivity ratio versus the human orexin-1 receptor. Ex vivo receptor binding studies demonstrated that JNJ-42847922 quickly occupied OX2R binding sites in the rat brain after oral administration and rapidly cleared from the brain. Seltorexant shows antidepressant and sleep-promoting effects in patients with major depressive disorder. JNJ-42847922 induces somnolence in healthy subjects without residual central effects.

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[1].

human OX2R: 8.0 (pKi); rat OX2R: 8.1 (pKi)

[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. DOI:10.1124/jpet.115.225466