利诺吡啶
| 中文名称 | 利诺吡啶 |
|---|---|
| 中文同义词 | 利诺吡啶;1,3-二氢-1-苯基-3,3-双(4-吡啶基甲基)-2H-吲哚-2-酮;利诺哌啶 |
| 英文名称 | 1,3-DIHYDRO-1-PHENYL-3,3-BIS(4-PYRIDINYLMETHYL)-2H-INDOL-2-ONE DIHYDROCHLORIDE |
| 英文同义词 | LINOPIRDINE DIHYDROCHLORIDE;1,3-DIHYDRO-1-PHENYL-3,3-BIS(4-PYRIDINYLMETHYL)-2H-INDOL-2-ONE DIHYDROCHLORIDE;LINOPIRDINE (DUP996);Linopirdine2HCl;DuP 996, 1,3-Dihydro-1-phenyl-3,3-bis(4-pyridinylmethyl)-2H-indol-2-one;1-Phenyl-3,3-bis(4-pyridinylmethyl)-2,3-dihydro-1H-indole-2-one;1-phenyl-3,3-bis(pyridin-4-ylmethyl)indolin-2-one;linopiridine |
| CAS号 | 105431-72-9 |
| 分子式 | C26H21N3O |
| 分子量 | 391.46 |
| EINECS号 | |
| 相关类别 | DuP 996;Pharmaceuticals;Potassium channel |
| Mol文件 | 105431-72-9.mol |
| 结构式 |  |
利诺吡啶 性质
| 熔点 | 186-186.5 °C |
|---|---|
| 沸点 | 655.9±50.0 °C(Predicted) |
| 密度 | 1?+-.0.06 g/cm3(Predicted) |
| 储存条件 | Desiccate at RT |
| 溶解度 | 二甲基亚砜：>10mg/mL |
| 酸度系数(pKa) | 6.01±0.10(Predicted) |
| 形态 | 结晶固体 |
| 颜色 | 白色至类白色 |
IC50: 2.4 μM (M-type K + current)
Linopirdine (DuP 996) inhibits IC (measured as a medium afterhyperpolarization tail current, ImAHP) with an IC
50
of 16.3 μM. Linopirdine (100 μM) weakly inhibits the K
+
leak current, IL, the transient outward current, IA, the delayed rectifier, IK, and the slow component of IAHP, by 28, 37, 36 and 52 percent, respectively. The mixed Na
+
/K
+
inward rectifying current, IQ, is essentially unaffected by Linopirdine (IC
50
>300 μM).
Linopirdine acts as an agonist of TRPV1 (transient receptor potential vanilloid type 1).
Linopirdine (DuP 996; i.v.; 0.1-6 mg/kg; increasing doses) transiently (10-15 min) and dose-dependently increases MAP by up to 15%.
| Animal Model: | Male Sprague-Dawley rats (300-350 g) |
| Dosage: | 0.1, 0.5, 1, 3, 6 mg/kg |
| Administration: | 5 intravenous bolus injections of increasing doses |
| Result: | Transiently and dose-dependently increases MAP by up to 15%. |
安全信息
| WGK Germany | 3 |
|---|