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ChemicalBook--->CAS DataBase List--->1293284-49-7

1293284-49-7

1293284-49-7 Structure

1293284-49-7 Structure
IdentificationBack 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
Chemical PropertiesBack Directory
[form ]

Solid
[color ]

Off-white to light yellow
Hazard InformationBack 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
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