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抑制剂描述:

产品名称:Lomerizine hydrochloride

产品别名:见爱必信

英文别名:Lomerizine hydrochloride

靶点:Calcium Channel

CAS:101477-54-7

纯度:>99%

外观:见爱必信

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Lomerizine dihydrochloride is a relatively new L- and T-type calcium channel blocker used in the treatment of migraine.

溶解性:Ethanol :49 mg/mL (90.5 mM)
DMSO :93 mg/mL (171.8 mM)

体外研究:

Lomerizine (0.1 μM and 1 μM) significantly reduces glutamate-induced neurotoxicity in rat cultured retinal neurons. Lomerizine (1 μM) also exhibits protective effects against both the N-methyl-D-aspartate and kainate induced types of neurotoxicity in rat cultured retinal neurons.

体内研究:Lomerizine (0.1 mg/kg and 1 mg/kg, i.v.) prior to ischemia and again immediately after reperfusion dose-dependently reduces the retinal damage in rat retina. Lomerizine (30 mg/kg, oral) reduces secondary necrosis at 2 weeks and secondary caspase-3 expression at 3 weeks in Piebald-Virol-Glaxo (PVG) rats. Lomerizine (30 mg/kg, oral) reduces morphological disruption, oxidative stress and phosphacan expression, and limits early increases in macrophage numbers in female PVG Hooded rats. Lomerizine (30 mg/kg, oral) protects RGCs from secondary death at 4 weeks but does not fully restore behavioural function (optokinetic nystagmus) in female PVG Hooded rats. Lomerizine (0.1 mg/kg or 0.3 mg/kg) significantly increases blood flow in the rabbit retina and optic nerve head (ONH), but blood flow changed little in the choroid or iris-ciliary body. Lomerizine (0.1 and 0.3 mg/kg, i.v.) significantly increases tissue blood flow in the optic nerve head and the putative blood flow in the long posterior ciliary artery with smaller reduction of blood pressure (0.3 mg/kg, i.v.) and without change in heart rate in rabbit. Lomerizine (0.1 and 0.3 mg/kg, i.v.) inhibits the hypoperfusion in the optic nerve head of rabbit.

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