Aranidipine

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Chemical Structure| 86780-90-7 同义名 : MPC1304
CAS号 : 86780-90-7
货号 : A577801
分子式 : C19H20N2O7
纯度 : 95%
分子量 : 388.37
MDL号 : MFCD00865813
存储条件:

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Aranidipine, a newly developed calcium antagonist, possesses unique pharmacologic characteristics in that its metabolite (M-1) still has antihypertensive action. During norepinephrine-induced constriction, the addition of aranidipine dilated both afferent and efferent arterioles in a dose-dependent manner; at 10-6 M, 83 +/- 6% and 90 +/- 6% reversal, respectively. Aranidipine has dilator action on both arterioles, whereas M-1 caused predominant dilation of afferent arterioles[3]. Administration of aranidipine 5-20 mg/d can effectively control blood pressure and is not inferior to retard-released felodipine 5-10 mg/d. The efficacy of 20 mg/d aranidipine is superior to that of retard-released felodipine 5-10 mg/d. And the effectiveness and safety of aranidipine are similar to those of retard-released felodipine[4]. When infused into the renal artery in anesthetized dogs, aranidipine (0.03 mg/kg/min) induced sustained increases in urine volume and urinary excretion of sodium and of potassium. Aranidipine (0.3, 1, and 3 mg/kg), when administered orally, dose-dependently increased urine volume and urinary excretion of electrolytes in conscious saline-loaded SHRs[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.87mL

2.57mL

1.29mL

25.75mL

5.15mL

2.57mL

参考文献

[1]Chen L, Jiang H, et al. [The effects of aranidipine on ambulatory blood pressures in patients with mild to moderate essential hypertension] . Zhonghua Nei Ke Za Zhi. 2013 Sep;52(9):749-52. Chinese.

[2]Masumiya H, Tanaka Y, et al. Inhibition of T-type and L-type Ca(2+) currents by aranidipine, a novel dihydropyridine Ca(2+) antagonist. Pharmacology. 2000 Aug;61(2):57-61.

[3]Nakamura A, Hayashi K, Fujiwara K, Ozawa Y, Honda M, Saruta T. Distinct action of aranidipine and its active metabolite on renal arterioles, with special reference to renal protection. J Cardiovasc Pharmacol. 2000 Jun;35(6):942-8

[4]Jiao Y, Chen L, Zheng JT, Ke YN, Wang Y, Yang HY, Jin H, Zhao XL, Liu MX, Wang L, Wang BY, Li DY. [Efficacy and safety of aranidipine in Chinese patients with mild-to-moderate essential hypertension]. Zhonghua Yi Xue Za Zhi. 2013 Oct 22;93(39):3104-10. Chinese

[5]Ichihara K, Okumura K, Kamei H, Nagasaka M, Kanda A, Kanno T, Miyoshi K, Miyake H. Renal effects of the calcium channel blocker aranidipine and its active metabolite in anesthetized dogs and conscious spontaneously hypertensive rats. J Cardiovasc Pharmacol. 1998 Feb;31(2):277-85