产品
编 号:F111960
分子式:C21H22FN7O
分子量:407.44
产品类型
结构图
CAS No: 1293281-49-8
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产品详情
生物活性:
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.
体内研究:
Seltorexant (JNJ-42847922) (3-30 mg/kg;口服) 剂量依赖性地诱导和延长雄性 Sprague-Dawley 大鼠的睡眠。 Seltorexant (30 mg/kg;口服;每天,持续 7 天) 在大鼠中的延长睡眠的作用在重复给药 7 天后维持不变。Animal Model:Male Sprague-Dawley rats (350-450 g)
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.