Lomerizine hydrochloride

Lomerizine hydrochloride Basic information
Product Name:Lomerizine hydrochloride
Synonyms:1-(4,4'-Difluorobenzhydryl)-4-(2,3,4-trimethoxybenzyl)piperazine·dihydrochloride;Flometizine hydrochloride;Lomerizine dihydrochloride, 99%, a new L- and T-type calcium channel blocker;Lomerizine2HCl;KB-2796 dihydrochloride;Piperazine, 1-[bis(4-fluorophenyl)methyl]-4-[(2,3,4-trimethoxyphenyl)methyl]-, hydrochloride (1:2);Lomerizine dihydrochloride, >=99%;1-(Bis(4-fluorophenyl)methyl)-4-(2,3,4-trimethoxybenzyl)piperazine dihydrochloride
CAS:101477-54-7
MF:C27H32Cl2F2N2O3
MW:541.46
EINECS:
Product Categories:Inhibitors;APIs;Heterocyclic Compounds;Intermediates & Fine Chemicals;Aromatics;Heterocycles;Neurochemicals;Pharmaceuticals
Mol File:101477-54-7.mol
Lomerizine hydrochloride Structure
Lomerizine hydrochloride Chemical Properties
Melting point 214-218°C dec.
storage temp. Inert atmosphere,2-8°C
solubility DMSO: ≥30mg/mL
form powder
color white to tan
Merck 14,5563
Stability:Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
CAS DataBase Reference101477-54-7(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
ToxicityLD50 orally in mice: 300 mg/kg (Ohtaka)
MSDS Information
Lomerizine hydrochloride Usage And Synthesis
DescriptionLomerizine 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 PropertiesColourless Crystalline Solid
OriginatorAkzo Nobel (Netherlands)
UsesA diphenylpiperazine calcium channel blocker. A selective cerebral vasodilator. Antimigraine.
Brand nameTeranas;Migsis
References1) Ishii?et al. (2009), Inhibitory effect of lomerizine, a prophylactic drug for migraines, on serotonin-induced contraction of the basilar artery; ?J. Pharmacol. Sci. 111 221 2)?Hara et al. (2004), Clinical potential of lomerizine, a Ca2+ channel blocker as an anti-glaucoma drug: effects on ocular circulation and retinal neuronal damage; Cardiovasc.Drug Rev. 22 199 3)?Ishii et al. (2011), Neuroprotection by lomerizine, a prophylactic drug for migraine, against hydrogen peroxide-induced hippocampal neurotoxicity; Mol. Cell Biochem. 358 1 4) Savigni?et al. (2013), Three Ca2+ channel inhibitors in combination limit chronic secondary degeneration following neurotrauma; ?Neuropharmacology 75 380 5) Tran?et al. (2014), The voltage-gated calcium channel blocker lomerizine is neuroprotective in motor neurons expressing mutant SOD, but not TDP-43; ?J. Neurochem. 130 455 6) O’Hare?et al. (2016), Specific combinations of ion channel inhibitors reduce excessive Ca2+ influx as a consequence of oxidative stress and increase neuronal and glial cell viability in vitro; ?Neuroscience 339 450
1-[1-(4-FLUORO-PHENYL)-ETHYL]-PIPERAZINE (R)-1-(4-Fluorophenyl)ethylamine (2,3-DIMETHOXY-6[[4-PHENYLMETHYL)-1-PIPERAZINYL]METHYL]PHENOL DIHYDROCHLORIDE 1-(4-METHOXY-BENZYL)-PIPERAZINE DIHYDROCHLORIDE 4,4'-Difluorobenzhydrylpiperazine 1-(4-FLUORO-ALPHA-PHENYLBENZYL)PIPERAZINE Belarizine (R)-1-(4-Fluorophenyl)ethylamine hydrochloride 1-(4-FLUORO-BENZYL)-PIPERAZINE 2HCL Lomerizine hydrochloride N-(BIS(4-FLUOROPHENYL)METHYL)PIPERAZINE DIHYDROCHLORIDE (R)-N-METHYL-1-(4-FLUOROPHENYL)ETHYLAMINE (4-fluorophenyl)(phenyl)methylamine Trimetazidine dihydrochloride (S)-1-(4-FLUOROPHENYL)ETHYLAMINE Lomerizine 1-(3,4-DIMETHOXY-BENZYL)-PIPERAZINE C-(4-FLUORO-PHENYL)-C-PHENYL-METHYLAMINE HYDROCHLORIDE

Email:[email protected] [email protected]
Copyright © 2024 Mywellwork.com All rights reserved.