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  • Cinnarizine
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Cinnarizine

A calcium channel inhibitor and histamine H4 receptor antagonist

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Cinnarizine的二维码
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  • 100mg
    ¥587.00
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  • 货号: ajci7632
  • CAS: 298-57-7
  • 别名: 桂利嗪
  • 分子式: C26H28N2
  • 分子量: 368.51
  • 纯度: >98%
  • 溶解度: DMF: 14 mg/ml,DMF:PBS(pH7.2) (1:2): 0.3 mg/mol,DMSO: 2 mg/ml,Ethanol: 3 mg/ml
  • 储存: Store at -20°C
  • 库存: 现货

Background

Cinnarizine is a calcium channel blocker.


Blockers of calcium channel are drugs disrupting the calcium movement via calcium channels, which are usually used as antihypertensive therapies to decrease blood pressure in hypertension patients.


In vitro: Previous study found that cinnarizine could inhibit the phosphorylation of both arterial myosin P-light chain and arterial actomyosin superprecipitation. Moreover, the concomitant inhibition of arterial superprecipitation and phosphorylation by perhexiline and cinnarizine was found to be similar to that of W-7. Such inhibitary effect was then characterized by a rightward shift in the pCa superprecipitation, depressed maximum activity as well as attenuation by exogenous calmodulin [1].


In vivo: Previous animal study showed that augmented effects were obtained in MES seizure model when cinnarizine was combined with sodium valproate. Whereas, in PTZ-induced seizures, augmented effects were obtained when nifedipine was combined with sodium valproate [2].


Clinical trial: The anti-vertigo effect of cinnarizine was evaluated in a double blinded, controlled study on fourty patients with well characterized peripheral or central vestibular disorders. Electronystagmography results did not show obviously detectable differences between patients treated with cinnarizine and placebo, and only a temporary depressant effect on vestibular nystagmus was observed in five healthy volunteers when cinnarizine dose was increased to 150 mg. In addition, cinnarizine was found to be generally well tolerated [3].

参考文献:
[1] Silver PJ,Dachiw J,Ambrose JM,Pinto PB.? Effects of the calcium antagonists perhexiline and cinnarizine on vascular and cardiac contractile protein function. J Pharmacol Exp Ther.1985 Sep;234(3):629-35.
[2] Brahmane RI,Wanmali VV,Pathak SS,Salwe KJ.? Role of cinnarizine and nifedipine on anticonvulsant effect of sodium valproate and carbamazepine in maximal electroshock and pentylenetetrazole model of seizures in mice. J Pharmacol Pharmacother.2010 Jul;1(2):78-81.
[3] Hausler R,Sabani E,Rohr M.? Effect of cinnarizine on various types of vertigo. Clinical and electronystagmographic results of a double-blind study. Acta Otorhinolaryngol Belg.1989;43(2):177-85.

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