新型正性肌力药物istaroxime研究进展

Advances in Istaroxime Research,a Novel Positive Inotropic Agent

充血性心力衰竭的患病率在全世界范围内持续上升,严重威胁着人们的生命健康。大量的研究表明细胞内钙离子代谢失调是心肌衰竭的主要生物化学标志,因此对心肌细胞内钙离子循环进行干预是治疗充血性心力衰竭的一种极富希望的方法。Istaroxime是一种新型正性肌力药物,它既可通过抑制钠钾三磷酸腺苷酶,增加细胞内游离钙离子浓度来实现其正性收缩作用,同时还可以通过提高肌浆网钙离子三磷酸腺苷酶的活性,加速细胞内游离钙离子清除而发挥正性舒张的作用。目前的研究显示istar-oxime是一种安全有效的正性肌力药物。

The prevalence of congestive heart failure （CHF） is continuously increasing worldwide. Abundant evidence points to a de- rangement in Ca2 ＋ cycling as the primary biochemical marker of the failing myocyte. Intervention of cardiocyte＇s Ca2 ＋ cycling is a promising therapeutic approach to the treatment of heart failure. As a novel positive inotropic agent, istaroxime has a dual action mechanism： inhibition of Na ＋ , K ＋ -ATPase and stimulation of sareoplasmie retieulum calcium ATPase isoform 2a （ SERCA2a）. The increase in cytoplasmic Ca2＋ due to Na ＋ , K ＋ -ATPase inhibition together with greater sarcoplasmic reticulum reloading results in both increased inotropy and lusitropy. Current reseach has indicated that istaroxime is a safe and effective positive inotropic agent.