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左西孟旦

左西孟旦用途

Levosimendan(OR1259)是钙增敏剂,通过与cardiac troponin C (cTnC)结合而发挥作用。

左西孟旦名称

[ CAS 号 ]:
141505-33-1

[ 中文名 ]:
左旋西孟旦

[ 英文名 ]:
Levosimendan

[中文别名 ]:

[英文别名 ]:

Levosimedan
Levosimendan
MFCD00867135
Simdax
(R)-Simendan

左西孟旦生物活性

[ 描述 ]:

Levosimendan(OR1259)是钙增敏剂,通过与cardiac troponin C (cTnC)结合而发挥作用。

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬

研究领域 >> 心血管疾病

[参考文献]

[1]. Nieminen, M.S., et al., Levosimendan: current data, clinical use and future development. Heart Lung Vessel, 2013. 5(4): p. 227-245.

[2]. Papp, Z., et al., Levosimendan: molecular mechanisms and clinical implications: consensus of experts on the mechanisms of action of levosimendan. Int J Cardiol, 2012. 159(2): p. 82-7.

[3]. Landoni, G., et al., Effects of levosimendan on mortality and hospitalization. A meta-analysis of randomized controlled studies. Crit Care Med, 2012. 40(2): p. 634-46.

[相关活性小分子]

左西孟旦物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 熔点 ]:
216-219ºC (dec.)

[ 分子式 ]:
C₁₄H₁₂N₆O

[ 分子量 ]:
280.285

[ 精确质量 ]:
280.107269

[ PSA ]:
113.43000

[ LogP ]:
0.59

[ 外观性状 ]:
黄色结晶粉末

[ 折射率 ]:
1.673

[ 储存条件 ]:
室温，干燥

左西孟旦安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H312-H332

[ 警示性声明 ]:
P280

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
R20/21/22

[ 安全声明 (欧洲) ]:
S36/S37

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
TY1570210

左西孟旦合成路线

详细合成路线

左西孟旦上下游产品

左西孟旦上游产品

左西孟旦下游产品

左西孟旦制备

在加热下,将(±)-6-(4-氨基苯基)-5-甲基哒嗪-3(2H)-酮(203g,1mol)溶于40ml异丙醇.然后缓慢加入L-酒石酸(300g,2rnol),在加热下搅拌至溶液澄清.在搅拌下缓慢冷却至室温,并在20℃搅拌过夜.过滤收集固体,并将其溶于水中,在搅拌下加入碳酸钾溶液(190g K2CO3溶于0.75ml水).过滤收集固体,水洗,干燥.在加热下将得到的104.6g固体溶于二氧六环,任其冷却至室温.过滤除去74.6g的消旋体,滤液减压浓缩至干,得23.8g结晶性固体的(-)-6-(4-氨基苯基)-5-甲基哒嗪-3(2H)-酮,纯度99.5%,熔点207～210℃,收率59.2%.
将(-)-6-(4-氨基苯基)-5-甲基哒嗪-3(2H)-酮和浓盐酸溶于水中,在搅拌和0～5℃下加入亚硝酸钠,10min后再加入丙二腈的水溶液,在室温搅拌1.5h.用乙酸钠将pH值调至6.0,过滤收集固体,用水和乙醇洗,得左西孟旦,熔点210～214℃,收率97%.

左西孟旦文献

Levosimendan exerts anti-inflammatory effects on cardiac myocytes and endothelial cells in vitro.

Thromb. Haemost. 113(2) , 350-62, (2015)

Levosimendan is a positive inotropic drug for the treatment of acute decompensated heart failure (HF). Clinical trials showed that levosimendan was particularly effective in HF due to myocardial infar...

Effect of levosimendan on the contractility of muscle fibers from nemaline myopathy patients with mutations in the nebulin gene.

Skelet. Muscle 5 , 12, (2015)

Nemaline myopathy (NM), the most common non-dystrophic congenital myopathy, is characterized by generalized skeletal muscle weakness, often from birth. To date, no therapy exists that enhances the con...

A Bayesian network meta-analysis on the effect of inodilatory agents on mortality.

Br. J. Anaesth. 114 , 746-56, (2015)

Inodilators are commonly used in critically ill patients, but their effect on survival has not been properly studied to date. The objective of this work was to conduct a network meta-analysis on the e...

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