162100-15-4
中文名称
6-氯-2,3-二氢-5-甲基-N-5-喹啉基-1H-吲哚-1-甲酰胺
英文名称
SB 215505
CAS
162100-15-4
分子式
C19H16ClN3O
分子量
337.8
MOL 文件
162100-15-4.mol
更新日期
2024/08/06 14:59:09
162100-15-4 结构式
基本信息
中文别名
化合物 T28680化合物 SB-215505
6-氯-5-甲基-N-(喹啉-5-基)二氢吲哚-1-甲酰胺
6-氯-2,3-二氢-5-甲基-N-5-喹啉基-1H-吲哚-1-甲酰胺
英文别名
SB 215505,SB2155056-Chloro-5-methyl-N-(quinolin-5-yl)indoline-1-carboxamide
6-chloro-5-methyl-N-quinolin-5-yl-2,3-dihydroindole-1-carboxamide
6-Chloro-2,3-dihydro-5-methyl-N-5-quinolinyl-1H-indole-1-carboxamide
1H-Indole-1-carboxamide, 6-chloro-2,3-dihydro-5-methyl-N-5-quinolinyl-
物理化学性质
沸点600.9±55.0 °C(Predicted)
密度1.385±0.06 g/cm3(Predicted)
储存条件2-8°C
溶解度DMSO: ~11 mg/mL at 60 °C, soluble
酸度系数(pKa)12.87±0.20(Predicted)
形态solid
颜色off-white
常见问题列表
生物活性
SB-215505 是一种有效的，亚型选择性 5-HT2B 受体拮抗剂，对 5-HT2B，5-HT2A，5-HT2C 的 pKi 值分别为 8.3、6.77、7.66。SB-215505 可以增加大鼠的清醒和运动活动。靶点
|
5-HT 2B Receptor 8.3 (pKi) |
5-HT 2A Receptor 6.77 (pKi) |
5-HT 2C Receptor 7.66 (pKi) |
体外研究
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.
体内研究
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. |