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HomeProduct name listLomerizine hydrochloride

Lomerizine hydrochloride

Synonym(s):1-[Bis(4-fluorophenyl)methyl]-4-[(2,3,4-trimethoxyphenyl)methyl]piperazine dihydrochloride

Lomerizine hydrochloride Structural

What is Lomerizine hydrochloride?

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)

The Uses of Lomerizine hydrochloride

A diphenylpiperazine calcium channel blocker. A selective cerebral vasodilator. Antimigraine.

What are the applications of Application

Lomerizine Hydrochloride is a calcium channel protein inhibitor

brand name

Teranas;Migsis

References

1) 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

Properties of Lomerizine hydrochloride

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 Reference 101477-54-7(CAS DataBase Reference)

Safety information for Lomerizine hydrochloride

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
ghs
Environment
GHS09
GHS Hazard Statements H302:Acute toxicity,oral
H410:Hazardous to the aquatic environment, long-term hazard
Precautionary Statement Codes P264:Wash hands thoroughly after handling.
P264:Wash skin thouroughly after handling.
P270:Do not eat, drink or smoke when using this product.
P273:Avoid release to the environment.
P391:Collect spillage. Hazardous to the aquatic environment
P301+P312:IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P501:Dispose of contents/container to..…

Computed Descriptors for Lomerizine hydrochloride

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