Levosimendan

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Chemical Structure| 141505-33-1 同义名 : Simsndan; OR-1259; simendan; Simadax; OR-1855; dextrosimendan; (-)-OR-1259; Levosimedan; Levosimendanum; Simdax; (R)-Simendan
CAS号 : 141505-33-1
货号 : A103792
分子式 : C14H12N6O
纯度 : 98%
分子量 : 280.29
MDL号 : MFCD00867135
存储条件：

Pure form Sealed in dry, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(178.39 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
描述 Levosimendan is a calcium sensitiser and potassium channel-opener used in the management of acutely decompensated congestive heart failure. The principal pharmacological effects of levosimendan are (a) increased cardiac contractility by calcium sensitisation of troponin C, (b) vasodilation, and (c) cardioprotection. Levosimendan also has favourable effects on neurohormone levels in heart failure patients. Levosimendan is generally well tolerated in acute heart failure patients: the most common adverse events encountered in this setting are hypotension, headache, atrial fibrillation, hypokalaemia and tachycardia[3]. Levosimendan increases contractile force of the heart and improves vasodilation. It increases the heart's sensitivity to calcium, thereby increasing cardiac contractility. Its mechanism of action is via the increased calcium sensitivity of myocytes by binding to cardiac troponin C in a calcium-dependent manner. Its opening of adenosine triphosphate-sensitive potassium channels in vascular smooth muscle leads to a vasodilatory effect and smooth muscle relaxatio[4]. Levosimendan possesses an isoform-selective phosphodiesterase-inhibitory effect[5]. Levosimendan might reduce mortality in cardiac surgery and cardiology settings of adult patients[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03281317 - Recruiting December 15, 2020 France ... 展开 >> CHU Amiens Picardie Recruiting Amiens, France, 80054 Contact: Pierre-Gregoire GUINOT 收起 <<
NCT03632837 Cardiac Arrest ... 展开 >> Resuscitation Inflammation Multi-Organ Disorder 收起 << Not Applicable Recruiting September 2019 Germany ... 展开 >> University Hospital Hamburg-Eppendorf Recruiting Hamburg, Germany, 20246 Contact: Jens Kubitz, Prof. Dr.    +49 (0) 40 7410 - 52415    j.kubitz@uke.de    Contact: Eike Pfefferkorn, Dr.       e.pfefferkorn@uke.de 收起 <<
NCT02627378 MERS-CoV Infection ... 展开 >> Refractory Hypoxemia 收起 << Phase 1 Completed - Saudi Arabia ... 展开 >> Dammam University KFHU Al-Khobar, EP, Saudi Arabia, 31952 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.57mL

0.71mL

0.36mL

17.84mL

3.57mL

1.78mL

35.68mL

7.14mL

3.57mL
参考文献

[1]Yokoshiki H, Katsube Y, et al. Levosimendan, a novel Ca2+ sensitizer, activates the glibenclamide-sensitive K+ channel in rat arterial myocytes. Eur J Pharmacol. 1997 Aug 27;333(2-3):249-59.

[2]Haikala H, Kaivola J, et al. Cardiac troponin C as a target protein for a novel calcium sensitizing drug, levosimendan. J Mol Cell Cardiol. 1995 Sep;27(9):1859-66.

[3]Nieminen MS, Fruhwald S, Heunks LM, Suominen PK, Gordon AC, Kivikko M, Pollesello P. Levosimendan: current data, clinical use and future development. Heart Lung Vessel. 2013;5(4):227-45

[4]Levin A, Paret G. Levosimendan. J Pediatr Intensive Care. 2013 Sep;2(3):95-103

[5]Papp Z, Édes I, Fruhwald S, De Hert SG, Salmenperä M, Leppikangas H, Mebazaa A, Landoni G, Grossini E, Caimmi P, Morelli A, Guarracino F, Schwinger RH, Meyer S, Algotsson L, Wikström BG, Jörgensen K, Filippatos G, Parissis JT, González MJ, Parkhomenko A, Yilmaz MB, Kivikko M, Pollesello P, Follath F. Levosimendan: molecular mechanisms and clinical implications: consensus of experts on the mechanisms of action of levosimendan. Int J Cardiol. 2012 Aug 23;159(2):82-7

[6]Landoni G, Biondi-Zoccai G, Greco M, Greco T, Bignami E, Morelli A, Guarracino F, Zangrillo A. Effects of levosimendan on mortality and hospitalization. A meta-analysis of randomized controlled studies. Crit Care Med. 2012 Feb;40(2):634-46