Molsidomine is an orally active, long acting vasodilating drug. Molsidomine is metabolized in the liver to the active metabolite linsidomine. Linsidomine is an unstable compound that releases nitric oxide (NO) upon decay as the actual vasodilating compound.
Molsidomine is a long-lasting, NO releasing vasodilator. It requires hepatic metabolism to be active, but causes no pharmacological tolerance. It is a useful antianginal. It has been shown to be enzymatically metabolized SIN-1 by the liver, then readily converted to active metabolite SIN-1A. It relaxes smooth muscle by activating GCS (soluble guanylate cyclase) which leads to increased cGMP formation.
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,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Kukovetz, W R., et al., 1986. Mode of action of nitrates with regard to vasodilatation and tolerance. Zeitschrift fυr Kardiologie. 75 Suppl 3(): 8-11.
[2] Kukovetz, W R., et al., 1985. Mechanism of vasodilation by molsidomine. American heart journal. 109(3 Pt 2): 637-40.
分子式 C9H14N4O4 |
分子量 242.23 |
CAS号 25717-80-0 |
储存方式 -20 ℃长期冷藏储存。冰袋运输 |
溶剂(常温) |
DMSO 48 mg/mL |
Water 13 mg/mL |
Ethanol 48 mg/mL |
体内溶解度
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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