|1-(Bis(4-氟苯基)甲基)-4-(2,3,4-三甲氧基苄基)哌嗪二盐酸盐|CsnPharm

CAS No.: 101477-54-7

Lomerizine 2HCl/盐酸洛美利嗪 Catalog No. CSN16682

Synonyms: KB-2796;Lomerizine (hydrochloride);B-2796

Lomerizine 2HCl is an L- and T-type calcium channel blocker used in the treatment of migraine.

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技术信息

生物活性

描述Lomerizine dihydrochloride (LOM) is a Ca2+ channel blocker used as an antimigraine drug, which is currently administered orally in Japan^[3]. Lomerizine reduced the retinal damage induced by NMDA (N-methyl-D-aspartate) and partially prevented the transsynaptic neuronal degeneration within dLGN and SC on the contralateral side. Moreover, lomerizine reduced the intravitreal NMDA induced decrease in the light-induced expression of c-Fos in the contralateral dLGN (used in this study to evaluate residual vision). Thus, lomerizine affords some protection against transsynaptic neuronal degeneration within the visual center of the mouse brain^[4]. Lomerizine may inhibit not only voltage-dependent Ca(2+) channels but also 5-HT(2A) receptors and so inhibit 5-HT-induced contraction in the basilar artery^[5]. The inhibition of H(2)O(2)-induced Ca(2+) influx through T-type VDCC (voltage-dependent Ca(2+) channel) seems to be important in the protective effect of lomerizine against oxidative stress. It is possible that lomerizine may be a useful drug for prophylactic treatment of migraine, because migraine is a risk factor for ischemic stroke^[6]. In healthy humans, lomerizine increased blood velocity in the optic nerve head, without significantly altering blood pressure or heart rate. Moreover, lomerizine reduced retinal damage in rats both in vitro and in vivo, presumably through a Ca(2+) channel blocking effect via an action that may involve a direct protection of retinal neurons as well as an improvement in the ocular circulation^[7].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8469 mL
- 9.2343 mL
- 18.4687 mL
- 5 mM
- 0.3694 mL
- 1.8469 mL
- 3.6937 mL
- 10 mM
- 0.1847 mL
- 0.9234 mL
- 1.8469 mL

技术信息

CAS号

101477-54-7

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H32Cl2F2N2O3

运输

蓝冰

分子量

541.46

别名

KB-2796;Lomerizine (hydrochloride);B-2796;Lomerizine HCl;盐酸洛美利嗪

溶解度

DMSO	110.0 mg/mL (203.2 mM)
Water	insoluble

动物实验配方

2% DMSO+water

5 mg/mL

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Lomerizine 2HCl/盐酸洛美利嗪 Catalog No. CSN16682

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