| Identification | Back Directory | [Name]
Seltorexant hydrochloride | [CAS]
1293284-49-7 | [Synonyms]
Seltorexant hydrochlorid
Seltorexant hydrochloride
JNJ-42847922 hydrochloride | [Molecular Formula]
C21H23ClFN7O | [MDL Number]
MFCD32690072 | [MOL File]
1293284-49-7.mol | [Molecular Weight]
443.91 |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
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] | | 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.
|
| [IC 50]
human OX2R: 8.0 (pKi); rat OX2R: 8.1 (pKi) | [References]
[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 |
|
|