中文名 | IPSU |
英文名 | IPSU |
别名 | 化合物IPSU |
英文别名 | IPSU 2-(1H-Indol-3-ylmethyl)-9-(4-methoxy-2-pyrimidinyl)-2,9-diazaspiro[5.5]undecan-1-one 2-((1H-indol-3-yl)methyl)-9-(4-methoxypyrimidin-2-yl)-2,9-diazaspiro[5.5]undecan-1-one 2,9-Diazaspiro[5.5]undecan-1-one, 2-(1H-indol-3-ylMethyl)-9-(4-Methoxy-2-pyriMidinyl)- |
CAS | 1373765-19-5 |
EINECS | 604-604-1 |
化学式 | C23H27N5O2 |
分子量 | 405.49 |
密度 | 1.32±0.1 g/cm3(Predicted) |
沸点 | 702.0±70.0 °C(Predicted) |
溶解度 | DMSO: ≥ 30 mg/mL |
酸度系数 | 16.94±0.30(Predicted) |
存储条件 | -20℃ |
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. |
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 . |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.466 ml | 12.331 ml | 24.661 ml |
5 mM | 0.493 ml | 2.466 ml | 4.932 ml |
10 mM | 0.247 ml | 1.233 ml | 2.466 ml |
5 mM | 0.049 ml | 0.247 ml | 0.493 ml |
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