Product Name: Lomerizine hydrochloride
Synonyms: 1-(4,4'-Difluorobenzhydryl)-4-(2,3,4-trimethoxybenzyl)piperazine·dihydrochloride;Flometizine hydrochloride;Lomerizine2HCl;Piperazine, 1-[bis(4-fluorophenyl)methyl]-4-[(2,3,4-trimethoxyphenyl)methyl]-, hydrochloride (1:2);Lomerizine dihydrochloride, >=99%;Lomerizine dihydrochloride, 99%, a new L- and T-type calcium channel blocker;1-(Bis(4-fluorophenyl)methyl)-4-(2,3,4-trimethoxybenzyl)piperazine dihydrochloride;1-(2,3,4-trimethoxybenzyl)-4-(bis(4-fluorophenyl)methyl)piperazinedihydrochl
CAS: 101477-54-7
MF: C27H32Cl2F2N2O3
MW: 541.46
EINECS:
Product Categories: Heterocyclic Compounds;Intermediates & Fine Chemicals;Neurochemicals;Pharmaceuticals;Aromatics;Heterocycles;Inhibitors;APIs
Mol File: 101477-54-7.mol
Lomerizine hydrochloride Structure
Lomerizine hydrochloride Chemical Properties
Melting point 214-218°C dec.
storage temp. -20°C Freezer
solubility DMSO: ≥30mg/mL
form powder
color white to tan
Merck 14,5563
CAS DataBase Reference 101477-54-7(CAS DataBase Reference)
Safety Information
Hazard Codes Xn,N
Risk Statements 22-50
Safety Statements 61
RIDADR UN 3077 9 / PGIII
WGK Germany 3
RTECS TK9189000
HS Code 29335990
Toxicity LD50 orally in mice: 300 mg/kg (Ohtaka)
MSDS Information
Lomerizine hydrochloride Usage And Synthesis
Description Lomerizine hydrochloride was introduced as Teranas and Migsis in Japan for the treatment of migraine. It is the first in its class of dual sodium and calcium channel blockers to be marketed for this indication. It can be synthetically obtained by reductive amination of 2,3,4-trimethoxybenzaldehyde with the appropiate benzhydryl piperazine. In dogs, Lomerizine exerts a potent, selective and long-lasting vasodilation of cerebral arteries related to a combination of mechanisms, especially a functional block of L-type voltagesensitive calcium channels (L-VSCCs). Lomerizine increases cerebral blood flow compared to peripheral blood flow with only weak effects on systemic arterial blood pressure. Other mechanisms involved could be blockade of other VSCC and sodium channels, 5-HT2 and alpha-1 receptors. As a reducing agent of cortical spreading depression and neurogenic inflammation, Lomerizine was shown to be useful in migraine. In an open clinical study, it demonstrated efficacy in the treatment of cluster headache. Moreover, it may have utility in other neurological diseases such as cerebrovascular ischemia or cerebral infarction.
Chemical Properties Colourless Crystalline Solid
Originator Akzo Nobel (Netherlands)
Uses A diphenylpiperazine calcium channel blocker. A selective cerebral vasodilator. Antimigraine.
Brand name Teranas;Migsis
China
