Lomerizine 2HCl

Catalog No.S4084 Synonyms: KB-2796

Lomerizine 2HCl Chemical Structure

Molecular Weight(MW): 541.46

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

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Biological Activity

Description Lomerizine dihydrochloride is a relatively new L- and T-type calcium channel blocker used in the treatment of migraine.
Targets
L-type calcium channel [1] T-type calcium channel [1]
In vitro

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. [1]

In vivo 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. [1] Lomerizine (30 mg/kg, oral) reduces secondary necrosis at 2 weeks and secondary caspase-3 expression at 3 weeks in adult Piebald-Virol-Glaxo (PVG) rats. [2] 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. [3] 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. [4] 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. [5]

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (184.68 mM)
Ethanol 52 mg/mL warmed (96.03 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+ddH2O
For best results, use promptly after mixing.
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 541.46
Formula

C27H30F2N2O3.2HCl

CAS No. 101477-54-7
Storage powder
in solvent
Synonyms KB-2796

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID