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2-(2-羟基-3-异丙氨基丙氧基)-5-(丙氧基甲基)苯乙酮的研究——一种潜在的肾上腺素能β受体阻滞剂,在给予异丙肾上腺素后对心肌线粒体功能的影响

[Study of 2-(2-hydroxy-3-isopropylaminopropoxy)-5-(propoxymethyl) acetophenone--a potential adrenoreceptor beta blocker affecting the function of myocardial mitochondria after administration of isoprenaline].

作者信息

Cizmáriková R, Gvozdjaková A, Kucharská J

机构信息

Farmaceutická fakulta Univerzity Komenského, Bratislava.

出版信息

Ceska Slov Farm. 1997 Oct;46(5):230-4.

PMID:9600145
Abstract

The present paper evaluated the effect of the potential beta-adrenoreceptor blocker 2-(3-isopropylamino-2-hydroxypropoxy)-5-(propoxymethyl) acetophenone (FoA33) on the oxidative and phosphorylating processes of the cardiac muscle influenced by small doses of isoprenaline (2 mg.kg-1). Under selected experimental conditions, the consumption of oxygen by the mitochondria of the cardiac muscle in states S3 and S4, rate of production of energy by mitochondria (OPR), coefficient of oxidative phosphorylyzation (ADP:O), respiratory control index (RCI) as well as the effect on the specific activity of the cytochromoxidase marker of mitochondria (COX) were examined. It follows from the obtained results that in contrast to large doses of isoprenaline (10-50 mg.kg-1) producing necrosis and affecting metabolic processes, small doses of isoprenaline (2 mg.kg-1) in many parameters activate the bioenergetic activity of the cardiac mitochondria, which is only minimally changed in combination with the beta-adrenoreceptor blocker (FoA33).

摘要

本文评估了潜在的β-肾上腺素能受体阻滞剂2-(3-异丙基氨基-2-羟基丙氧基)-5-(丙氧基甲基)苯乙酮(FoA33)对小剂量异丙肾上腺素(2mg.kg-1)影响下心肌氧化和磷酸化过程的作用。在选定的实验条件下,检测了心肌线粒体在S3和S4状态下的耗氧量、线粒体能量产生速率(OPR)、氧化磷酸化系数(ADP:O)、呼吸控制指数(RCI)以及对线粒体细胞色素氧化酶标记物(COX)比活性的影响。从获得的结果可以看出,与大剂量异丙肾上腺素(10 - 50mg.kg-1)导致坏死并影响代谢过程不同,小剂量异丙肾上腺素(2mg.kg-1)在许多参数上激活了心肌线粒体的生物能量活性,而与β-肾上腺素能受体阻滞剂(FoA33)联合使用时,这种活性仅有微小变化。

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[Study of 2-(2-hydroxy-3-isopropylaminopropoxy)-5-(propoxymethyl) acetophenone--a potential adrenoreceptor beta blocker affecting the function of myocardial mitochondria after administration of isoprenaline].2-(2-羟基-3-异丙氨基丙氧基)-5-(丙氧基甲基)苯乙酮的研究——一种潜在的肾上腺素能β受体阻滞剂,在给予异丙肾上腺素后对心肌线粒体功能的影响
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