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A7643958

LomerizineDihydrochloride , 10mMinDMSO , 101477-54-7

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

CAS NO.:101477-54-7

Empirical Formula: C27H32Cl2F2N2O3

Molecular Weight: 541.46

MDL number: MFCD01703867

Pack Size Price Stock Quantity
1ml RMB159.20 In Stock
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Update time: 2022-07-08

PRODUCT 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 Reference 101477-54-7(CAS DataBase Reference)

Description and Uses

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.

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

Safety

Symbol(GHS) 
GHS07,GHS09
Signal word  Warning
Hazard statements  H302-H410
Precautionary statements  P264-P270-P273-P301+P312-P391-P501
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)

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