Quinidine是一种发现于金鸡纳树树皮和根皮的天然生物碱,是 K+ 通道 (K+ channel) 的有效阻断剂,其 IC50 值为 19.9 μM。Quinidine可用于疟疾的相关研究。
Quinidine 是一种抗心律失常剂,也是 K+ 通道 (K+ channel) 的有效阻断剂,其 IC50 值为 19.9 μM。Quinidine is a stereoisomer of quinine, originally derived from the bark of the cinchona tree. Quinidine is used to treat abnormal heart rhythms. Like all other class I antiarrhythmic agents, quinidine primarily works by blocking the fast inward sodium current. At micromolar concentrations, quinidine inhibits Na+/K+-ATPase by binding to the same receptor sites as the digitalis glycosides such as ouabain. Quinidine is also used to treat malaria. The half life of oral quinidine is 6 to 8 hours, and it is eliminated by the cytochrome P450 system in the liver. About 20% is excreted unchanged via the kidneys. Quinidine is also an inhibitor of the cytochrome P450 enzyme 2D6, and can lead to increased blood levels of lidocaine, Beta blockers, opioids, and some anti-depressants. Quinidine also inhibits the transport protein P-glycoprotein and so can cause some peripherally acting drugs such as loperamide to have CNS side effects such as respiratory depression if the two drugs are co-administered.
分子量 | 324.42 |
分子式 | C20H24N2O2 |
CAS号 | 56-54-2 |
溶解性(25°C) | DMSO 50 mg/mL |
储存条件 | 2-8°C, protect from light, sealed |
运输方式 | 冰袋运输,根据产品的不同,可能会有相应调整。 |
*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前,需考虑其在不同溶剂中的溶解度限制。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 3.0824 mL | 15.4121 mL | 30.8242 mL |
5 mM | 0.6165 mL | 3.0824 mL | 6.1648 mL |
10 mM | 0.3082 mL | 1.5412 mL | 3.0824 mL |
小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
动物 A的Km系数 |
例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。
[1] Laura Vitali Serdoz, et al. Quinidine-A legacy within the modern era of antiarrhythmic therapy
[3] Felix Yang, et al. Quinidine revisited
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