CARABERSAT
| 中文名称 | CARABERSAT |
|---|---|
| 中文同义词 | 卡拉博沙;化合物 T14863 |
| 英文名称 | Carabersat |
| 英文同义词 | Carabersat;Benzamide, N-[(3R,4S)-6-acetyl-3,4-dihydro-3-hydroxy-2,2-dimethyl-2H-1-benzopyran-4-yl]-4-fluoro- |
| CAS号 | 184653-84-7 |
| 分子式 | C20H20FNO4 |
| 分子量 | 357.38 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 184653-84-7.mol |
| 结构式 |  |
CARABERSAT 性质
| 沸点 | 559.3±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.31±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 形态 | 固体 |
| 酸度系数(pKa) | 13.05±0.60(Predicted) |
| 颜色 | 白色至米白色 |
[ 3 H]Carabersat ([ 3 H]SB 204269) binds to rat forebrain membranes with moderate affinity (K d 40 nM) and pK i values of 7.3. Carabersat is able to bind to mouse forebrain membranes, and the binding is saturable and stereospecific, with a K d of 53 nM. The labelled [ 3 H]Carabersat produces a K d of 32 nM. Carabersat (SB-204269, 1-100 μM) has no effect on Na + current in cultured hippocampal neurones. Carabersat also shows no effect on action potential discharges evoked by elevating external K + . Carabersat (SB-204269) is structurally-related to the benzopyran ATP-sensitive potassium channel (KATP) opener, cromakalim, but has opposite stereochemistry, and the mechanism of action of Carabersat is not thought to involve KATP.
Carabersat (5b) significantly elevates anticonvulsant activity in mice.