Hydralazine HCl是Hydralazine (Apresoline)的盐酸盐形式,是直接有效的平滑肌松弛剂,IC50为1.9 mM。
Hydralazine hydrochloride is a hydrochloride salt of hydralazine (Apresoline) that is a direct-acting smooth muscle relaxant with an IC50 of 1.9 mM. Hydralazine (Apresoline) is used to treat high blood pressure. Hydralazine hydrochloride works by relaxing the blood vessels so that blood can flow more easily through the body. Hydralazine hydrochloride increases guanosine monophosphate levels, decreasing the action of the second messenger IP3, limiting calcium release from the sarcoplasmic reticulum of smooth muscle. This results in vessel relaxation. Hydralazine hydrochloride dilates arterioles more than veins. Hydralazine hydrochloride recently has been identified as a nitric oxide donor. Activation of hypoxia-inducible factors has been suggested as a mechanism. Hydralazine hydrochloride relaxes vascular smooth muscles of arteries and arterioles, causing peripheral vasodilation and decreasing peripheral vascular resistance. These actions decrease blood pressure and increase heart rate, stroke volume, and cardiac output.
分子量 | 196.64 |
分子式 | C8H8N4.HCl |
CAS号 | 304-20-1 |
性状 | Solid |
溶解性(25°C) | DMSO |
储存条件 |
粉末型式 -20°C 3年;4°C 2年 溶于溶剂 -80°C 6个月;-20°C 1个月 |
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 | 5.0854 mL | 25.4272 mL | 50.8544 mL |
5 mM | 1.0171 mL | 5.0854 mL | 10.1709 mL |
10 mM | 0.5085 mL | 2.5427 mL | 5.0854 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。
[2] Kimberly S Collins, et al. Genotype-Guided Hydralazine Therapy
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