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A new positive inotropic drug levosimendan Research Progress
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A new positive inotropic drug levosimendan Research Progress
Levosimendan as a new positive inotropic drugs - a calcium-sensitizing agent, owing to its ability to increase cardiac contractility without increasing heart rate and myocardial oxygen consumption, etc., are considered very promising clinical application of new drugs. In this paper, the role of levosimendan in recent years, the mechanism, pharmacological effects and clinical application of such things as a review.
First, the mechanism of levosimendan
At present the clinical application of positive inotropic drugs are mainly catecholamine class and phosphodiesterase inhibitors, which are ultimately within the myocardial cells by increasing the concentration of Ca2 to set off a chain reaction, thereby increasing the myocardial cells contractility. Levosimendan is different, it does not directly increase the intracellular calcium ion concentration or increased cardiac troponin and with Ca2 affinity, but rather on the thin filament cardiac troponin C (Tnc) combination of the amino acid N-terminal increase Tnc and Ca2 conformational stability of the complexes. Tnc combined with Ca2, the original myosin molecular conformation changed to lift it for the muscle fiber protein and cross-bridge combined with each other impediment. Cross-bridge binding and thin filament, filament twist occurs, myocardial fiber contraction. In addition, with other calcium-sensitizing agent in both systolic and diastolic acting on the Tnc and Ca2 complexes are different and Tnc Levosimendan was a combination of Ca2 concentration-dependent, that is, when the myocardial cells at high concentration within the Ca2 (myocardial cell contraction time) it Tnc high affinity, while the myocardial concentration of intracellular Ca2 low (myocardial cells, relaxation time) with low affinity Tnc. Therefore, it is the role of strong systolic and diastolic period, the role of weak, so to prevent or mitig
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