Lomerizine is an inhibitor of voltage-gated L-type and T-type Ca2+ channels as well as transient receptor potential (TRP5) channels. Lomerizine is clinically used to treat migraine and vertigo. Lomerizine exhibits neuroprotective benefit in animal models of amyotrophic lateral sclerosis (ALS), decreasing glutamate excitotoxicity, Ca2+ overload, and mitochondrial dysfunction. In other animal models, lomerizine protects against NMDA-induced retinal damage and neurodegeneration.
| Cas No. | 101477-54-7 |
|---|---|
| Purity | ≥98% |
| Formula | C27H30F2N2O3 • 2HCl |
| Formula Wt. | 541.47 |
| Chemical Name | 1-[Bis(4-fluorophenyl)methyl]-4-[(2,3,4-trimethoxyphenyl)methyl]piperazine dihydrochloride |
| IUPAC Name | 1-[bis(4-fluorophenyl)methyl]-4-[(2,3,4-trimethoxyphenyl)methyl]piperazine;dihydrochloride |
| Synonym | Lomerizine dihydrochloride |
| Melting Point | 204-207°C |
| Appearance | White or off-White Crystalline Powder |
| Store Temp | Ambient |
|---|---|
| Ship Temp | Ambient |
| MSDS | L5751 MSDS PDF |
|---|---|
| Info Sheet | L5751 Info Sheet PDF |
Tran LT, Gentil BJ, Sullivan KE, et al. The voltage-gated calcium channel blocker lomerizine is neuroprotective in motor neurons expressing mutant SOD1, but not TDP-43. J Neurochem. 2014 Apr 9. [Epub ahead of print]. PMID: 24716897.
Inoue Y, Yabe T. Lomerizine therapy for the treatment of benign paroxysmal vertigo of childhood transitioning into atypical basilar migraine: A case report. Exp Ther Med. 2013 Jun;5(6):1573-1575. PMID: 23837033.
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 Apr;16(2):103-14. PMID: 19788586.
Fitzgerald M, Bartlett CA, Harvey AR, Dunlop SA. Early events of secondary degeneration after partial optic nerve transection: an immunohistochemical study. J Neurotrauma. 2010 Feb;27(2):439-452. PMID: 19852581.
