依利色林
| 中文名称 | 依利色林 |
|---|---|
| 中文同义词 | (Z,E)-1-(2-氟苯基)-3-(4-羟基苯基)-2-丙烯-1-酮 O-[2-(二甲基氨基)乙基]肟;依利色林;化合物 T11217 |
| 英文名称 | Eplivanserin |
| 英文同义词 | EPLIVANSERIN;(Z,E)-1-(2-Fluorophenyl)-3-(4-hydroxyphenyl)-2-propen-1-one O-[2-(dimethylamino)ethyl]oxime;VAIOZOCLKVMIMN-PRJWTAEASA-N;5-hydroxytryptamine Receptor,Serotonin Receptor,5-HT2A,5-HT Receptor,Eplivanserin,SR46349,oral,dopamine,SR 46349,Inhibitor,inhibit,release;2-Propen-1-one, 1-(2-fluorophenyl)-3-(4-hydroxyphenyl)-, O-[2-(dimethylamino)ethyl]oxime, (1Z,2E)- |
| CAS号 | 130579-75-8 |
| 分子式 | C19H21FN2O2 |
| 分子量 | 328.38 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 130579-75-8.mol |
| 结构式 |  |
依利色林 性质
| 沸点 | 453.4±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.08 |
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 9.60±0.15(Predicted) |
|
5-HT 2 Receptor 5.8 nM (IC 50 , in rat cortical membrane) |
5-HT 2 Receptor 1.14 nM (Ki) |
Eplivanserin is a potent, selective and orally available 5-HT 2 antagonist, with an IC 50 of 5.8 nM in rat cortical membrane, and a K d of 1.14 nM. Eplivanserin hemifumarate (SR 46349B) shows weak inhibition on other 5-HT kinases, with IC 50 s of 0.12 μM (Pig cortex 5-HT 1C ), 14 μM (Rat hippocampus 5-HT 1A ), and 16 μM (Rat stnatum 5-HT 1B , Ox caudate nucleus 5-HT 1D ). Eplivanserin also has inhibitory effects on rat cortex adrenergic α 1 and α 2 , rat whole brain histammine H 1 , Na + channel, and rat striatum dopamine D 1 and D 2 , with IC 50 s of 3.4 μM, 1.0 μM, 5.0 μM, 39 μM, 9 μM and 28 μM, respectively.
Eplivanserin hemifumarate (SR 46349B) inhibits 5-HT 2 receptor binding of [ 3 H]ketanserin with an ED 50 of 0.087 mg/kg after i.p. injection, and 0.097 mg/kg after p.o administration in mice.