生物活性

Na–H exchange (NHE) represents an important mechanism for mediating such injury. NHE represents an important mechanism for the development of myocardial ischemic and reperfusion injury and inhibitors have been consistently shown to protect the ischemic and reperfused heart by correcting the ionic imbalance associated with this form of pathological insult. Cariporide is a potent NHE inhibitor.

In vitro: Cariporide concentration dependently inhibited the amiloride sensitive sodium influx in rabbit erythrocytes, reduced the swelling of human platelets caused by intracellular acidification, and delayed pH recovery in rat cardiomyocytes.

In vivo: In anaesthetised rats undergoing coronary artery ligation intravenous and oral pretreatment with Cariporide caused a dose dependent reduction or a complete prevention of ventricular premature beats, ventricular fibrillation, and ventricular tachycardia. The compound was well tolerated and neutral to circulatory variables.

Clinical trial: Cariporide has been evaluated in a large dose-finding Phase II/Phase III clinical trial to assess the efficacy in patients with acute coronary syndromes. Overall results failed to demonstrate protection but sub-group analysis revealed significant risk reductions with the highest cariporide dose especially in high risk patients undergoing coronary artery bypass surgery.

体外研究

体内研究

激酶实验

细胞实验

动物实验

0.1-1 mM

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

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。

参考文献

[1] Yang X, et al. J Surg Res. 2013 Dec;185(2):797-804.
[2] Wu S, et al. Pharmacology. 2013; 91(3-4):123-30.

体内溶解度

Clinical Trial Information ( data from http://clinicaltrials.gov )

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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