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临床医学中的生物能量学十五。临床使用的β受体肾上腺素能阻滞剂对辅酶Q10-酶的抑制作用。

Bioenergetics in clinical medicine XV. Inhibition of coenzyme Q10-enzymes by clinically used adrenergic blockers of beta-receptors.

作者信息

Kishi T, Watanabe T, Folkers K

出版信息

Res Commun Chem Pathol Pharmacol. 1977 May;17(1):157-64.

PMID:17892
Abstract

Adrenergic blockers for beta-receptors were studied for inhibition of mitochrondrial CoQ10-enzymes. These enzymes are indispensable for the bioenegetics of the myocardium. Propranolol is frequently used to treat hypertension; in some patients, it depresses myocardial function as an adverse reaction. This side effect may be related to the inhibition by propranolol of CoQ10-enzymes of the myocardium. Timolol showed negligible inhibition of the CoQ10-enzyme, NADH-oxidase. Metoprolol was less inhibitory than propranolol. Five alprenolols showed inhibition which approached that of propranolol. The 1-isomer of alprenolol showed weak inhibition of another CoQ10-enzyme, succinoxidase, but the other beta-blockers were essentially non-inhibitory to this enzyme. The drug of choice is timolol, based on negligible inhibition of these bioenergetic enzymes of the heart, which correlates with its pharmacologically low cardiac depressant effects.

摘要

对β受体肾上腺素能阻滞剂进行了研究,以考察其对线粒体辅酶Q10酶的抑制作用。这些酶对于心肌的生物能量学来说是不可或缺的。普萘洛尔常用于治疗高血压;在一些患者中,它作为一种不良反应会抑制心肌功能。这种副作用可能与普萘洛尔对心肌辅酶Q10酶的抑制作用有关。噻吗洛尔对辅酶Q10酶NADH氧化酶的抑制作用可忽略不计。美托洛尔的抑制作用比普萘洛尔弱。五种阿普洛尔的抑制作用接近普萘洛尔。阿普洛尔的1-异构体对另一种辅酶Q10酶琥珀酸氧化酶的抑制作用较弱,但其他β受体阻滞剂对该酶基本无抑制作用。基于对心脏这些生物能量酶的抑制作用可忽略不计,噻吗洛尔是首选药物,这与其药理学上较低的心脏抑制作用相关。

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