JNJ-42847922
JNJ-42847922 Basic information
- Product Name:
- JNJ-42847922
- Synonyms:
-
- [2-(4,6-DIMETHYLPYRIMIDIN-2-YL)-1,3,3A,4,6,6A-HEXAHYDROPYRROLO[3,4-C]PYRROL-5-YL]-[2-FLUORO-6-(TRIAZOL-2-YL)PHENYL]METHANONE
- JNJ-42847922
- JNJ-42847922,Cid 67116280
- [5-(4,6-dimethyl-pyrimidin-2-yl)-hexahydro-pyrrolo[3,4-c]pyrrol-2-yl]-(2-fluoro-6-[1,2,3]triazol-2-yl-phenyl)-methanone
- Methanone, [5-(4,6-dimethyl-2-pyrimidinyl)hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl][2-fluoro-6-(2H-1,2,3-triazol-2-yl)phenyl]-
- Seltorexant (JNJ-42847922)
- Hypocretin Receptor,JNJ42847922,HCRT Receptor,Orexin Receptor (OX Receptor),Seltorexant,movement,barrier,insomnia,somnolence,eye,blood-brain,inhibit,rapid,selective,sleep,JNJ 42847922,Inhibitor
- (5-(4,6-Dimethylpyrimidin-2-yl)hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)(2-fluoro-6-(2H-1,2,3-triazol-2-yl)phenyl)methanone
- CAS:
- 1293281-49-8
- MF:
- C21H22FN7O
- MW:
- 407.44
- Product Categories:
-
- API
- Mol File:
- 1293281-49-8.mol
JNJ-42847922 Chemical Properties
- Boiling point:
- 667.7±65.0 °C(Predicted)
- Density
- 1.46±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: 250 mg/mL (613.59 mM)
- pka
- 6.50±0.50(Predicted)
- form
- Solid
- color
- White to yellow
JNJ-42847922 Usage And Synthesis
Description
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.
Uses
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 Seltorexant (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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