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首页> 外文期刊>Canadian Journal of Physiology and Pharmacology >The myosin activator omecamtiv mecarbil: a promising new inotropic agent
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The myosin activator omecamtiv mecarbil: a promising new inotropic agent

机译：肌球蛋白激活剂omecamtiv mecarbil：一种有前途的新型正性肌力药

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Heart failure became a leading cause of mortality in the past few decades with a progressively increasing prevalence. Its current therapy is restricted largely to the suppression of the sympathetic activity and the renin-angiotensin system in combination with diuretics. This restrictive strategy is due to the potential long-term adverse effects of inotropic agents despite their effective influence on cardiac function when employed for short durations. Positive inotropes include inhibitors of the Na+/K+ pump, beta-receptor agonists, and phosphodiesterase inhibitors. Theoretically, Ca2+ sensitizers may also increase cardiac contractility without resulting in Ca2+ overload; nevertheless, their mechanism of action is frequently complicated by other pleiotropic effects. Recently, a new positive inotropic agent, the myosin activator omecamtiv mecarbil, has been developed. Omecamtiv mecarbil binds directly to beta-myosin heavy chain and enhances cardiac contractility by increasing the number of the active force-generating cross-bridges, presumably without major off-target effects. This review focuses on recent in vivo and in vitro results obtained with omecamtiv mecarbil, and discusses its mechanism of action at a molecular level. Based on clinical data, omecamtiv mecarbil is a promising new tool in the treatment of systolic heart failure.
机译：在过去的几十年中，心力衰竭已成为导致死亡的主要原因，其患病率也在逐步提高。其目前的疗法在很大程度上限于与利尿剂联用时抑制交感活性和肾素-血管紧张素系统。这种限制性策略是由于正性肌力药物潜在的长期不良作用，尽管短期使用它们对心脏功能有有效影响。正性肌力药包括Na + / K +泵抑制剂，β受体激动剂和磷酸二酯酶抑制剂。从理论上讲，Ca2 +增敏剂也可以增加心脏收缩能力，而不会导致Ca2 +过载。然而，它们的作用机理常常由于其他多效性作用而变得复杂。最近，已经开发出一种新的正性肌力药，即肌球蛋白激活剂omecamtiv mecarbil。 Omecamtiv mecarbil直接与β-肌球蛋白重链结合，并通过增加产生主动力的跨桥的数量来增强心脏收缩力，大概没有重大的脱靶效应。这篇综述着重于使用omecamtiv mecarbil获得的近期体内和体外结果，并讨论了其在分子水平上的作用机理。根据临床数据，omecamtiv mecarbil是治疗收缩性心力衰竭的有前途的新工具。

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