8-OH-DPAT
8-OH-DPAT 性质
| 沸点 | 372.5±42.0 °C(Predicted) |
|---|---|
| 密度 | 1.03±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 150mg/ml DMSO 溶液 |
| 形态 | 固体 |
| 酸度系数(pKa) | 10.54±0.40(Predicted) |
| 颜色 | 白色 |
| 旋光性 (optical activity) | [α]25/D 67.8° in methanol(lit.) |
8-OH-DPAT 用途与合成方法
|
5-HT 1A Receptor 8.19 (pIC 50 ) |
5-HT 7 Receptor 466 nM (Ki) |
8-OH-DPAT is a potent and selective 5-HT agonist, with a pIC 50 of 8.19 for 5-HT1A; weakly binds to 5-HT1B (pIC 50 , 5.42), 5-HT (pIC 50 <5). 8-OH-DPAT has high affinity at 5-HT7 with a K i of 466 nM, and does not bind to 5-HT6 or 5-HT4.
8-OH-DPAT (1 mg/kg) normalizes hypolocomotion, significantly increases wakefulness and reduces the duration of REM sleep without effect on the duration of non-REM sleep in the dark period in orexin knockout (KO) mice. 8-OH-DPAT shows no obvious effect on wakefulness or the duration of either REM sleep or non-REM sleep in WT mice. 8-OH-DPAT (1 mg/kg, s.c.) activates 5-HT1A receptor in orexin knockout mice.
