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Merck

L6295

Sigma-Aldrich

Lomerizine dihydrochloride

≥98% (HPLC), powder

Sinónimos:

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

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About This Item

Fórmula empírica (notación de Hill):
C27H30F2N2O3·2HCl
Número de CAS:
Peso molecular:
541.46
Número MDL:
Código UNSPSC:
12352200
ID de la sustancia en PubChem:
NACRES:
NA.25

Análisis

≥98% (HPLC)

formulario

powder

color

white to tan

solubilidad

DMSO: ≥30 mg/mL

temp. de almacenamiento

2-8°C

cadena SMILES

Cl.Cl.COc1ccc(CN2CCN(CC2)C(c3ccc(F)cc3)c4ccc(F)cc4)c(OC)c1OC

InChI

1S/C27H30F2N2O3.2ClH/c1-32-24-13-8-21(26(33-2)27(24)34-3)18-30-14-16-31(17-15-30)25(19-4-9-22(28)10-5-19)20-6-11-23(29)12-7-20;;/h4-13,25H,14-18H2,1-3H3;2*1H

Clave InChI

LOGVKVSFYBBUAJ-UHFFFAOYSA-N

Acciones bioquímicas o fisiológicas

Lomerizine dihydrochloride is a voltage-dependent calcium channel blocker and selective cerebral vasodilator. It is one of the most selective calcium channel blockers for the CNS and cerebral arteries. It has been reported to inhibit both T-type and L-type Ca2+ currents in rat hippocampal CA1 pyramidal neurons, to prevent glutamate-induced neurotoxicity in rat hippocampal primary cell cultures, and to exhibit protective effects in animal models of migraine, ischemia and hypoxia. In Japan, lomerizine has been used as the first-line prophylactic drug for migraines.

Pictogramas

Exclamation markEnvironment

Palabra de señalización

Warning

Frases de peligro

Clasificaciones de peligro

Acute Tox. 4 Oral - Aquatic Acute 1 - Aquatic Chronic 1

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable


Certificados de análisis (COA)

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N Shiraki et al.
Biological & pharmaceutical bulletin, 24(5), 555-557 (2001-05-31)
Acquired resistance to chemotherapy is a major problem during cancer treatment. One mechanism for drug resistance is overexpression of the MDR (multidrug resistance)1 gene encoding the transmembrane efflux pump, P-glycoprotein (P-gp). Calcium channel blockers such as verapamil, nifedipine and nicardipine
Melinda Fitzgerald et al.
Investigative ophthalmology & visual science, 50(11), 5456-5462 (2009-05-29)
After partial optic nerve (ON) injury, intact retinal ganglion cells (RGCs) undergo secondary death, but the topographic distribution of this death is unknown, and it is unclear which cell death pathways are involved. Although the calcium channel blocker lomerizine reduces
Kiyoshi Negoro
Brain and nerve = Shinkei kenkyu no shinpo, 61(10), 1135-1141 (2009-11-04)
Calcium channel antagonists have been employed in the prophylactic treatment of migraine. Their major action is the inhibition of Ca2+ influx into smooth muscle cells that is mediated through high voltage-sensitive Ca2+ channels. These drugs had been introduced for the
Tomoko Hibino et al.
Journal of pharmacological sciences, 108(1), 89-94 (2008-09-09)
The effects of goshuyuto and chotosan, traditional Japanese medicines, on collagen-induced platelet aggregation were examined using guinea-pig blood. Goshuyuto at the concentration of 1,000 mug/mL inhibited collagen-induced platelet hyper-aggregation to the same degree as aspirin at the concentration of 100
Bian-Sheng Ji et al.
Acta pharmacologica Sinica, 27(4), 414-418 (2006-03-17)
To investigate the modulatory effect of CJZ3, a lomerizine derivative, on P-glycoprotein (P-gp) function in rat brain microvessel endothelial cells (RBMEC). RBMEC were isolated and cultured in Dulbecco modified Eagle medium/F12 (1:1) medium, and the amount of intracellular rhodamine 123

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