Endogenous Cardiotonics: Search and Problems.

Arkady R Kolpakov, Roman A Knyazev
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Abstract

Medicinal preparations currently used for the treatment of patients with chronic cardiac failure involve those that reduce the heart load (vasodilators, diuretics, beta-blockers, and angiotensin-converting enzyme (ACE) inhibitors). Cardiotonic drugs with the cAMP-dependent mechanism are unsuitable for long-term administration due to the intensification of metabolic processes and an increase in the oxygen demand of the myocardium and all tissues of the body. For many years, digoxin has remained the only preparation enhancing the efficiency of myocardial performance. The detection of digoxin and ouabain in intact animals has initiated a search for other compounds with cardiotonic activity. The review summarizes current data on the effect exerted on the heart performance by endogenous compounds, from simple, such as NO and CO, to steroids, fatty acids, polypeptides, and proteins. Controversial questions and problems with the introduction of scientific achievements into clinical practice are discussed. The results obtained by the authors and their colleagues after many years of studies on the cardiotropic properties of serum lipoproteins are also reported. The experimentally established cardiotonic activity of apoprotein A-1, which is accompanied by a decrease in the relative consumption of oxygen, maybe of great interest.
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内源性强心剂:研究和问题。
目前用于治疗慢性心力衰竭患者的药物制剂包括那些降低心脏负荷的药物(血管扩张剂、利尿剂、-受体阻滞剂和血管紧张素转换酶(ACE)抑制剂)。具有camp依赖机制的强心药物,由于代谢过程的加剧和心肌及身体各组织需氧量的增加,不适合长期给药。多年来,地高辛一直是提高心肌功能效率的唯一制剂。地高辛和瓦巴因在完整动物体内的检测开启了对其他具有强心剂活性的化合物的研究。这篇综述总结了目前关于内源性化合物对心脏功能影响的数据,从简单的一氧化氮和一氧化碳到类固醇、脂肪酸、多肽和蛋白质。讨论了有争议的问题和将科学成果引入临床实践的问题。本文还报道了作者及其同事对血清脂蛋白的致心性进行多年研究后得到的结果。实验证实载脂蛋白a -1的强心活性伴随着相对耗氧量的减少,这可能是非常有趣的。
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来源期刊
Cardiovascular and Hematological Disorders - Drug Targets
Cardiovascular and Hematological Disorders - Drug Targets Medicine-Cardiology and Cardiovascular Medicine
CiteScore
1.90
自引率
0.00%
发文量
36
期刊介绍: Cardiovascular & Hematological Disorders - Drug Targets aims to cover all the latest and outstanding developments on the medicinal chemistry, pharmacology, molecular biology, genomics and biochemistry of contemporary molecular targets involved in cardiovascular and hematological disorders e.g. disease specific proteins, receptors, enzymes, genes. Each issue of the journal contains a series of timely in-depth reviews written by leaders in the field covering a range of current topics on drug targets involved in cardiovascular and hematological disorders. As the discovery, identification, characterization and validation of novel human drug targets for cardiovascular and hematological drug discovery continues to grow.
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