6-氯-2,3-二氢-5-甲基-N-5-喹啉基-1H-吲哚-1-甲酰胺
| 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 |
|---|---|
| 中文同义词 | 6-氯-2,3-二氢-5-甲基-N-5-喹啉基-1H-吲哚-1-甲酰胺;6-氯-5-甲基-N-(喹啉-5-基)二氢吲哚-1-甲酰胺;化合物 T28680;化合物 SB-215505 |
| 英文名称 | SB 215505 |
| 英文同义词 | 6-Chloro-2,3-dihydro-5-methyl-N-5-quinolinyl-1H-indole-1-carboxamide;6-chloro-5-methyl-N-quinolin-5-yl-2,3-dihydroindole-1-carboxamide;1H-Indole-1-carboxamide, 6-chloro-2,3-dihydro-5-methyl-N-5-quinolinyl-;6-Chloro-5-methyl-N-(quinolin-5-yl)indoline-1-carboxamide;SB 215505,SB215505;6-Chloro-5-methyl-N-(quinolin-5-yl)indoline-1-carboxamide , SB-215505 |
| CAS号 | 162100-15-4 |
| 分子式 | C19H16ClN3O |
| 分子量 | 337.8 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 162100-15-4.mol |
| 结构式 |  |
6-氯-2,3-二氢-5-甲基-N-5-喹啉基-1H-吲哚-1-甲酰胺 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/mLat 60 °C |
| 形态 | 固体 |
| 酸度系数(pKa) | 12.87±0.20(Predicted) |
| 颜色 | 米白色 |
| InChI | 1S/C19H16ClN3O/c1-12-10-13-7-9-23(18(13)11-15(12)20)19(24)22-17-6-8-21-16-5-3-2-4-14(16)17/h2-6,8,10-11H,7,9H2,1H3,(H,21,22,24) |
| InChIKey | BPVGSWDWIRIUME-UHFFFAOYSA-N |
| SMILES | Cc1cc2CCN(C(=O)Nc3ccnc4ccccc34)c2cc1Cl |
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。
|
5-HT 2B Receptor 8.3 (pKi) |
5-HT 2A Receptor 6.77 (pKi) |
5-HT 2C Receptor 7.66 (pKi) |
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.
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. |
安全信息
| WGK Germany | 3 |
|---|---|
| 存储类别 | 13 - 不可燃性固体 |