产品
编 号:F141898
分子式:C23H27N5O2
分子量:405.49
产品类型
结构图
CAS No: 1373765-19-5
联系客服
产品详情
生物活性:
IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85.
体内研究:
IPSU has low blood clearance, shows high maximal blood exposure and AUC after oral dosing. It exhibits an acceptable absolute oral bioavailability and a brain/blood concentration ratio that indicated favorable brain penetration. IPSU increases sleep when dosed during the mouse active phase (lights off); IPSU induces sleep primarily by increasing NREM sleep. IPSU shows a fast onset of action, with a clear increase in total sleep time during the first hour afterdosing. The effect lasts 4-5 h, after which time the total sleep time per hour is the same as on vehicle day .
体外研究:
Orexin receptor antagonists represent attractive targets for the development of drugs for the treatment of insomnia. IPSU binds rapidly and reaches equilibrium very quickly in binding and/or functional assays.