162100-15-4
162100-15-4 結(jié)構(gòu)式
常見(jiàn)問(wèn)題列表
生物活性
SB-215505 是一種有效的，亞型選擇性 5-HT2B 受體拮抗劑，對(duì) 5-HT2B，5-HT2A，5-HT2C 的 pKi 值分別為 8.3、6.77、7.66。SB-215505 可以增加大鼠的清醒和運(yùn)動(dòng)活動(dòng)。靶點(diǎn)
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5-HT 2B Receptor 8.3 (pKi) |
5-HT 2A Receptor 6.77 (pKi) |
5-HT 2C Receptor 7.66 (pKi) |
體外研究
SB-215505 is 30 fold selective for the 5-HT 2B over the 5-HT 2A receptor, and only marginally selective over the 5-HT 2C receptor.
體內(nèi)研究
SB-215505 (0.1-1.0 mg/kg; i.p.; two doses) dose-dependently increases wakefulness (W) and decreases IS, PS, SWS-2.
| Animal Model: | Male Sprague-Dawley rats weighing 230-260 g |
| Dosage: | 0.1, 0.3 and 1.0 mg/kg |
| Administration: | IP; two doses (4 days between two doses) |
| Result: | Dose-dependently increased wakefulness (W) and decreased intermediate stage of sleep (IS), paradoxical sleep (PS), SWS-2. |