利诺吡啶
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 |
利诺吡啶 用途与合成方法
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%. |
