产品
编 号:F195711
分子式:C22H18F4N6O
分子量:458.41
产品类型
结构图
CAS No: 1628843-99-1
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产品详情
生物活性:
JNJ-54717793, as a brain penetrant, is an orally active, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasma EC50=85 ng/mL). The Ki values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders.
体内研究:
JNJ-5471779 (30 mg/kg; p.o.; 6 hours) significantly reduces the latency for rapid eye movement (REM) sleep and prolongs the time spent in REM sleep.JNJ-5471779 (3~30 mg/kg; p.o.) attenuates bradycardia responses.JNJ-5471779 (5mg/kg; p.o.) shows low clearance.Animal Model:OX2R KO mice
Dosage:30 mg/kg
Administration:P.o.
Result:Significantly reduced the latency for rapid eye movement (REM) sleep and prolonged the time spent in REM sleep.
Animal Model:Rat
Dosage:3~30 mg/kg
Administration:P.o.
Result:Attenuated bradycardia responses.
Animal Model:Mouse
Dosage:5.0 mg/kg (Pharmacokinetic Analysis)
Administration:P.o.
Result:Clearance was found to be low.