Bioactivity | 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]. | ||||||||||||
In Vivo | Seltorexant (JNJ-42847922) (3-30 mg/kg; p.o.) dose-dependently induces and prolongs sleep in male Sprague-Dawley rats[1].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[1]. Animal Model: | ||||||||||||
Name | Seltorexant | ||||||||||||
CAS | 1293281-49-8 | ||||||||||||
Formula | C21H22FN7O | ||||||||||||
Molar Mass | 407.44 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
|
||||||||||||
Reference | [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. |