Effects of class I antiarrhythmic drugs on mitochondrial ATPase activity in guinea pig heart preparations.

General pharmacology Pub Date : 1993-01-01 DOI:10.1016/0306-3623(93)90040-5

A A Almotrefi

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引用次数: 6

Abstract

1. The effects of three class I antiarrhythmic drugs quinidine, lidocaine and lorcainide on undamaged myocardial mitochondrial ATPase [ATP: phosphohydrolase, EC 3.6.1.3] activity were evaluated in guinea pig heart preparations. 2. All three drugs inhibited the enzyme activity in a concentration-dependent fashion. 3. Lorcainide was the most potent, exerting inhibitory effects in the range of less than 1.0 nM-2.0 mM, with IC20 and IC50 values of 9.4 +/- 0.6 nM and 87.2 +/- 5.5 microM. However, in the range of approx. 10 nM-10 microM, the enzyme response decreased only slightly with increasing lorcainide concentrations. 4. Quinidine and lidocaine, on the other hand, inhibited the enzyme activity in the range of 1.0 microM-100 mM. 5. The IC20 and IC50 values for quinidine were 0.92 +/- 0.04 mM and 4.8 +/- 0.6 mM and for lidocaine were 115 +/- 6 microM and 2.3 +/- 0.3 mM. 6. The results show that all three drugs inhibit mitochondrial ATPase activity and that lorcainide is the most potent. 7. These inhibitory effects may be related to the lipophilicity and membrane stabilizing activity of this class of antiarrhythmic drugs.

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一类抗心律失常药物对豚鼠心脏制剂中线粒体atp酶活性的影响。

1. 在豚鼠心脏制剂中，评价了3种I类抗心律失常药物奎尼丁、利多卡因和氯卡奈德对未损伤心肌线粒体ATP酶[ATP:磷酸水解酶，EC 3.6.1.3]活性的影响。2. 所有三种药物都以浓度依赖性的方式抑制酶活性。3.氯卡奈德的抑制作用最强，在1.0 nM-2.0 mM范围内，IC20值为9.4 +/- 0.6 nM, IC50值为87.2 +/- 5.5微米。然而，在大约的范围内。10 nM-10 μ m时，随着氯卡胺浓度的增加，酶反应略有下降。4. 而奎尼丁和利多卡因在1.0 μ m ~ 100 μ m范围内对酶活性有抑制作用。奎尼丁的IC20和IC50分别为0.92 +/- 0.04 mM和4.8 +/- 0.6 mM，利多卡因的IC20和IC50分别为115 +/- 6微米和2.3 +/- 0.3毫米。结果表明，这三种药物都能抑制线粒体atp酶的活性，其中氯卡奈德的作用最有效。7. 这些抑制作用可能与该类抗心律失常药物的亲脂性和膜稳定活性有关。

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General pharmacology

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