(R)-(-)-Niguldipine hydrochloride是α1 拮抗剂, L-type Ca2+ 通道阻断剂。Niguldipine hydrochloride的对映体之一。
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] Graziadei et al (1989) Stereoselective binding of niguldipine enantiomers to alpha1A-adrenoceptors labeled with [3H]5-methyl-urapidil. Eur.J.Pharmacol. 172 329. PMID: 2555206.
[2] Boer et al (1989) (+)-Niguldipine binds with very high affinity to Ca2+ channels and to a subtype of alpha1-adrenoceptor. Eur.J.Pharmacol. 172 131. PMID: 2548881.
[3] Hollt et al (1992) Stereoisomers of calcium antagonists which differ markedly in their potencies as calcium blockers are equally effective in modulating drug transport by P-glycoprotein. Biochem.Pharmacol. 43 2601. PMID: 1352973.
[4] Wetzel et al (1995) Discovery of alpha1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine. J.Med.Chem. 38 1579. PMID: 7752182.
分子式 C36H39N3O6.HCl |
分子量 646.18 |
CAS号 113145-70-3 |
储存方式 ﹣20 ℃长期储存。冰袋运输 |
溶剂(常温) |
DMSO |
Water 10 mM |
Ethanol |
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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