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Merck
CN

L6295

Lomerizine dihydrochloride

≥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:
分子量:
541.46
NACRES:
NA.25
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
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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

SMILES string

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

InChI key

LOGVKVSFYBBUAJ-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

color

white to tan

solubility

DMSO: ≥30 mg/mL

storage temp.

2-8°C

Quality Level

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

Exclamation markEnvironment

signalword

Warning

hcodes

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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分析证书(COA)

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Yasuhiro Tamaki et al.
Investigative ophthalmology & visual science, 44(11), 4864-4871 (2003-10-28)
To investigate the effects of lomerizine, a Ca2+ antagonist, on the ocular tissue circulation in rabbits and on the circulation in the optic nerve head (ONH) and choroid in healthy volunteers. Lomerizine (0.1 [n=10] or 0.3 [n=11] mg/kg) or vehicle
Toshiki Mizuno et al.
Clinical neuropharmacology, 32(2), 113-116 (2009-06-11)
A 64-year-old woman was admitted to our hospital for recurrent stroke and cognitive impairment and was diagnosed with cerebral autosomal dominant arteriopathy with subcortical infarcts and leukoencephalopathy (CADASIL). Iodine-123 iodoamphetamine single photon emission computed tomography showed hypoperfusion in the whole
Bian-Sheng Ji et al.
Die Pharmazie, 65(7), 515-519 (2010-07-29)
P-Glycoprotein, a 170-180 kDa membrane glycoprotein that mediates multidrug resistance, hydrolyses ATP to efflux a broad spectrum of hydrophobic agents. To observe the interaction of a P-gp reversal agent with P-gp ATPase activity should provide further insights into the mechanisms
Melinda Fitzgerald et al.
Experimental neurology, 216(1), 219-230 (2009-01-03)
Secondary degeneration is a form of 'bystander' damage that can affect neural tissue both nearby and remote from an initial injury. Partial optic nerve transection is an excellent model in which to unequivocally differentiate events occurring during secondary degeneration from
Luan T Tran et al.
Journal of neurochemistry, 130(3), 455-466 (2014-04-11)
Excitotoxicity and disruption of Ca(2+) homeostasis have been implicated in amyotrophic lateral sclerosis (ALS) and limiting Ca(2+) entry is protective in models of ALS caused by mutation of SOD1. Lomerizine, an antagonist of L- and T-type voltage-gated calcium channels and

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