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L6295

Lomerizine dihydrochloride

Name: Lomerizine dihydrochloride
Brand: SIGMA

≥98% (HPLC), powder

别名:

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

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关于此项目

经验公式（希尔记法）:

C₂₇H₃₀F₂N₂O₃·2HCl

化学文摘社编号:

101477-54-7

分子量:

541.46

NACRES:

NA.25

PubChem Substance ID:

329817637

UNSPSC Code:

12352200

MDL number:

MFCD01703867

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

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属性

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to tan

solubility

DMSO: ≥30 mg/mL

storage temp.

2-8°C

SMILES string

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

InChI key

LOGVKVSFYBBUAJ-UHFFFAOYSA-N

说明

Biochem/physiol Actions

Lomerizine dihydrochloride is a voltage-dependent calcium channel blocker and selective cerebral vasodilator.

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.

pictograms

GHS07,GHS09

signalword

Warning

hcodes

H302,H410

pcodes

P264 - P270 - P273 - P301 + P312 - P391 - P501

Hazard Classifications

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

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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Secondary retinal ganglion cell death and the neuroprotective effects of the calcium channel blocker lomerizine.

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

Increase in doxorubicin cytotoxicity by inhibition of P-glycoprotein activity with lomerizine.

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

CJZ3, a lomerizine derivative, modulates P-glycoprotein function in rat brain microvessel endothelial cells.

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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全球贸易项目编号

货号	GTIN
L6295-10MG	04061833958735
L6295-50MG	04061833234846