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Cinepazide Maleate

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Chemical Structure| 26328-04-1 同义名 : MD-67350
CAS号 : 26328-04-1
货号 : A469349
分子式 : C26H35N3O9
纯度 : 98%
分子量 : 533.571
MDL号 : MFCD01320526
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(196.79 mM)，配合低频超声助溶，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

H2O: 50 mg/mL(93.71 mM)，配合低频超声助溶
动物实验配方：

PO 0.5% CMC-Na 80 mg/mL clear

生物活性
靶点

  • Calcium Channel
描述 Cinepazide Maleate (CM) is a vasodilator. Among various concentrations, 10 μM CM exhibited most significant protection on PC12 cells against OGD (oxygen-glucose deprivation) injury. CM was found to suppress OGD-induced oxidative stress, as supported by its capability of reducing intracellular reactive oxygen species and malondialdehyde production and enhancing superoxide dismutase activity. CM can protect neuronal cells against OGD injury by preserving mitochondrial functions[2]. T2D (type 2 diabetes) exacerbated CCH-induced (chronic cerebral hypoperfusion) brain damage and cognitive impairment, and CM (cinepazide maleate) ameliorated these effects[1]. Cinepazide (3 - 30 mg/kg, i.v.) produced a dose-related and transient increase in vertebral, carotid, renal and femoral arterial flow as well as cardiac output and a decrease in total peripheral resistance in anesthetized dogs. Cinepazide resembled cinnarizine and papaverine in that the drug antagonized rabbit aortic contraction induced by KCl, norepinephrine or CaCl2[3]. Cinepazide in concentrations ranging from 10(-6) to 10(-5) M augmented the relaxing responses to ATP, adenosine and cAMP. Cinepazide slightly reduced the 3H-efflux evoked by electrical stimulation. However, the relaxing response was mostly augmented by the treatment with cinepazide[4]. Cinepazide maleate combined with edaravone can effectively increase the survival rate of brain cells and promote the volatilization of neurological function in the treatment of hemorrhage in the subretinal space of the omentum[5].
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
NCT01831011 Acute Ischemic Stroke Phase 2 Completed - China, Shanxi ... 展开 >> the Department of Neurology Xi an, Shanxi, China, 710032 收起 <<
NCT01851759 Ischemic Stroke Phase 2 Unknown August 2014 China, Shaanxi ... 展开 >> Xijing Hospital Not yet recruiting Xi'an, Shaanxi, China, 710032 Contact: Gang Zhao    02984775361    zhaogang@fmmu.edu.cn 收起 <<
NCT01946919 - Unknown June 2014 -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.87mL

0.37mL

0.19mL

9.37mL

1.87mL

0.94mL

18.74mL

3.75mL

1.87mL
参考文献

[1]Li Y, Zhang T, Zhang X, Zou W, Gong X, Fu J. Cinepazide Maleate Improves Cognitive Function and Protects Hippocampal Neurons in Diabetic Rats with Chronic Cerebral Hypoperfusion. Biol Pharm Bull. 2017;40(3):249‐255

[2]Zhao J, Bai Y, Zhang C, et al. Cinepazide maleate protects PC12 cells against oxygen-glucose deprivation-induced injury. Neurol Sci. 2014;35(6):875‐881

[3]Akashi A, Hirohashi M, Suzuki I, Shibamura S, Kasahara A. Nihon Yakurigaku Zasshi. 1979;75(5):507‐516

[4]Muramatsu I, Sakakibara Y, Hong SC, Fujiwara M. Effects of cinepazide on the purinergic responses in the dog cerebral artery. Pharmacology. 1984;28(1):27‐33

[5]Cai Z, Zhang H, Song H, Piao Y, Zhang X. Edaravone combined with cinepazide maleate on neurocyte autophagy and neurological function in rats with subarachnoid hemorrhage. Exp Ther Med. 2020;19(1):646‐650