research use only
Cat.No.S4084
| Related Targets | CFTR CRM1 CD markers AChR Sodium Channel Potassium Channel GABA Receptor TRP Channel ATPase GluR |
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| Other Calcium Channel Inhibitors | Bay K 8644 Nilvadipine Flunarizine 2HCl Cilnidipine YM-58483 (BTP2) Imperatorin Manidipine 2HCl Astragaloside A Benidipine HCl Azelnidipine |
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In vitro |
DMSO
: 8 mg/mL
(14.77 mM)
Ethanol : 3 mg/mL Water : Insoluble |
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In vivo |
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| Molecular Weight | 541.46 | Formula | C27H30F2N2O3.2HCl |
Storage (From the date of receipt) | |
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| CAS No. | 101477-54-7 | Download SDF | Storage of Stock Solutions |
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| Synonyms | KB-2796 | Smiles | COC1=C(C(=C(C=C1)CN2CCN(CC2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F)OC)OC.Cl.Cl | ||
| Targets/IC50/Ki |
L-type calcium channel
T-type calcium channel
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| In vitro |
Lomerizine (0.1 μM and 1 μM) significantly reduces glutamate-induced neurotoxicity in rat cultured retinal neurons. Lomerizine (1 μM) also exhibits protective effects against both the N-methyl-D-aspartate and kainate induced types of neurotoxicity in rat cultured retinal neurons.
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| In vivo |
Lomerizine (0.1 mg/kg and 1 mg/kg, i.v.) prior to ischemia and again immediately after reperfusion dose-dependently reduces the retinal damage in rat retina. Lomerizine (30 mg/kg, oral) reduces secondary necrosis at 2 weeks and secondary caspase-3 expression at 3 weeks in adult Piebald-Virol-Glaxo (PVG) rats. Lomerizine (30 mg/kg, oral) reduces morphological disruption, oxidative stress and phosphacan expression, and limits early increases in macrophage numbers in female PVG Hooded rats. Lomerizine (30 mg/kg, oral) protects RGCs from secondary death at 4 weeks but does not fully restore behavioural function (optokinetic nystagmus) in female PVG Hooded rats. Lomerizine (0.1 mg/kg or 0.3 mg/kg) significantly increases blood flow in the rabbit retina and optic nerve head (ONH), but blood flow changed little in the choroid or iris-ciliary body. Lomerizine (0.1 and 0.3 mg/kg, i.v.) significantly increases tissue blood flow in the optic nerve head and the putative blood flow in the long posterior ciliary artery with smaller reduction of blood pressure (0.3 mg/kg, i.v.) and without change in heart rate in rabbit. Lomerizine (0.1 and 0.3 mg/kg, i.v.) inhibits the hypoperfusion in the optic nerve head of rabbit.
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References |
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