Cinepazide - CAS 23887-46-9
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Not Intended for Therapeutic Use. For research use only.
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Cinepazide is a vasodilator. Cinepazide (30 mg/kg, i.v.) potentiated the vertebral vasodilator response of dogs to intravertebral adenosine and cyclic AMP, Intravertebral cinepazide(1-10 mg) increased vertebral blood flow in a dose-related manner and the effect was partially inhibited by intravenous pretreatment with aminophylline but not by pretreatment with autonomic antagonists. Cinepazide resembled cinnarizine and papaverine in that the drug antagonized rabbit aortic contraction induced by KCl, norepinephrine or CaCl2. Cinepazide in concentrations ranging from 10-6 to 10-5M augmented the relaxing responses to ATP, adenosine and cAMP. However, this agent did not affect the relaxations induced by isoproterenol and papaverine and the contractions induced by 5-HT, prostaglandin F2α and ATP. cinepazide selectively potentiates the relaxing response mediated through purinergic P1 receptors.
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1.Cinepazide maleate protects PC12 cells against oxygen-glucose deprivation-induced injury.
Zhao J1, Bai Y, Zhang C, Zhang X, Zhang YX, Chen J, Xiong L, Shi M, Zhao G. Neurol Sci. 2014 Jun;35(6):875-81. doi: 10.1007/s10072-013-1618-z. Epub 2013 Dec 29.
Our previous study showed that cinepazide maleate (CM) was as effective and safe as mildronate in the treatment of acute ischemic stroke in a randomized, double-blind, active-controlled phase II multicenter trial, but underlying mechanism(s) is not well understood. As an extending study, here we demonstrated that CM could protect neuronal cells by affecting mitochondrial functions. PC12 cells were exposed to 2.5 h oxygen-glucose deprivation (OGD) followed by a 24 h reoxygenation, and then treated with different concentrations (1, 10, 100 μM) of CM. Among various concentrations, 10 μM CM exhibited most significant protection on PC12 cells against OGD 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. Importantly, our results showed that CM could preserve mitochondrial functions, as revealed by its capability of stabilizing mitochondrial membrane potential, improving OGD-induced suppression of mitochondrial respiratory complex activities and enhancing ATP production.
2.High performance liquid chromatographic method for the determination of cinepazide maleate and its application to a pharmacokinetic study in rats.
Zhao J1, Song Y1, Wang H2, Sun Y1, Liu M1, Lu C1, Li Y1, Wang S1, Zhu X1, Hai W1, Wen A3, Jia Y4. J Chromatogr B Analyt Technol Biomed Life Sci. 2014 Apr 15;957:105-9. doi: 10.1016/j.jchromb.2014.02.038. Epub 2014 Mar 4.
A simple and reliable high performance liquid chromatographic (HPLC) method has been developed and validated to quantify cinepazide maleate, a calcium blocker, in rat plasma. Cinepazide maleate and Tinidazole (internal standard) have been extracted by a simple liquid-liquid extraction before injection into chromatographic system. Chromatographic separation was achieved on a reversed phase C18 column with a mobile phase consisted of a water mixture of 10mM potassium dihydrogen phosphate (pH=4.5):methanol (40:60, v/v), pumped at flow rate of 1.0mL/min, and detected at 303nm. The method exhibited a linear range of 0.12-120μg/mL in blank rat plasma, with the lower detection limit of 0.06μg/mL. The method was statistically validated for linearity, accuracy, precision, selectivity and stability following FDA guidelines. The intra- and inter-assay coefficients of variation did not exceed ±15% from the nominal concentration. The accuracy of cinepazide maleate was within ±15% of the theoretical value.
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CAS 23887-46-9 Cinepazide

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