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Lomerizine 2HCl

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Chemical Structure| 101477-54-7 同义名 : 洛美利嗪二盐酸盐 ;KB-2796;Lomerizine (hydrochloride);Lomerizine HCl;B 2796;Lomerizine dihydrochloride
CAS号 : 101477-54-7
货号 : A163797
分子式 : C27H32Cl2F2N2O3
纯度 : 98%
分子量 : 541.457
MDL号 : MFCD01703867
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(221.62 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
动物实验配方：

2% DMSO+water 5 mg/mL

生物活性
靶点

  • Calcium Channel
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.85mL

0.37mL

0.18mL

9.23mL

1.85mL

0.92mL

18.47mL

3.69mL

1.85mL
参考文献

[1]Furuishi T, Kato Y, et al. Effect of terpenes on the skin permeation of lomerizine dihydrochloride. J Pharm Pharm Sci. 2013;16(4):551-63.

[2]Meister S, Frey B, et al. Calcium channel blocker verapamil enhances endoplasmic reticulum stress and cell death induced by proteasome inhibition in myeloma cells. Neoplasia. 2010 Jul;12(7):550-61.

[3]Furuishi T, Kato Y, Fukami T, et al. Effect of terpenes on the skin permeation of lomerizine dihydrochloride. J Pharm Pharm Sci. 2013;16(4):551‐563

[4]Ito Y, Nakamura S, Tanaka H, et al. Lomerizine, a Ca2+ channel blocker, protects against neuronal degeneration within the visual center of the brain after retinal damage in mice. CNS Neurosci Ther. 2010;16(2):103‐114

[5]Ishii M, Kobayashi S, Ohkura M, Yamamoto R, Shimizu S, Kiuchi Y. Inhibitory effect of lomerizine, a prophylactic drug for migraines, on serotonin-induced contraction of the basilar artery. J Pharmacol Sci. 2009;111(2):221‐225

[6]Ishii M, Iizuka R, Kiuchi Y, Mori Y, Shimizu S. Neuroprotection by lomerizine, a prophylactic drug for migraine, against hydrogen peroxide-induced hippocampal neurotoxicity. Mol Cell Biochem. 2011;358(1-2):1‐11

[7]Hara H, Toriu N, Shimazawa M. Clinical potential of lomerizine, a Ca2+ channel blocker as an anti-glaucoma drug: effects on ocular circulation and retinal neuronal damage. Cardiovasc Drug Rev. 2004;22(3):199‐214