All AbMole products are for research use only, cannot be used for human consumption.
Lomerizine dihydrochloride is a relatively new L- and T-type calcium channel blocker used in the treatment of migraine. Lomerizine inhibits the low- and high-voltage activated Ca2+ currents in dissociated rat brain neurons at a threshold concentration of 0.01 μM and IC50 of 1.9 μM and H2O2-induced Ca2+ influx in hippocampal neurons is inhibited by 1 μM Lomerizine. Pre-treatment with 1 μM Lomerizine significantly reduces acute death of motor neurons in spinal cord-DRG cultures exposed to 50 μM glutamate, a concentration that kills approximately 40% of motor neurons in the culture by 6 h, and inhibits the rise in cytosolic [Ca2+] that occurs with glutamate treatment. 0.5 μM Lomerizine is sufficient to significantly prevent the mitochondrial fragmentation of mitochondria induced by SOD1G93A.
 |
Source | J Neurochem (2014). Figure 6. Lomerizine hydrochloride |
| Method | Motor neuron viability | |
| Cell Lines | motor neurons | |
| Concentrations | 0.5 μM | |
| Incubation Time | 5 d | |
| Results | TDP-43 was predominantly cytoplasmic in a significantly greater percentage of motor neurons expressing the mutants relative to TDP-43WT, but the proportion was not significantly affected by treatment with lomerizine |
 |
Source | J Neurochem (2014). Figure 3. Lomerizine hydrochloride |
| Method | Mitochondrial length and transport | |
| Cell Lines | motor neurons | |
| Concentrations | 0.5 μM | |
| Incubation Time | 24 h | |
| Results | Treatment with lomerizine prevented the increase in mitochondrial [Ca2+] that occurred by 1 day following microinjection of plasmid encoding SOD1G93A-eGFP (Fig. 3a), as well as the decrease in Dw |
| Cell Experiment | |
|---|---|
| Cell lines | Motor neurons |
| Preparation method | A stock solution of 100 mM lomerizine was prepared in dimethyl sulfoxide (DMSO) and aliquots were stored at −80°C. Lomerizine was further diluted to 400 μM in DMSO prior to use and further diluted in culture medium to working concentrations. |
| Concentrations | 400 μM |
| Incubation time | 3 d |
| Animal Experiment | |
|---|---|
| Animal models | Male adult C57BL/6J mice |
| Formulation | water containing 5% arabic gum |
| Dosages | 30 mg/kg |
| Administration | p.o. |
| Molecular Weight | 541.46 |
| Formula | C27H30F2N2O3.2HCl |
| CAS Number | 101477-54-7 |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Calcium Channel Products |
|---|
| CBD3063
CBD3063 is a selective, first-in-class, CRMP2-based peptidomimetic small molecule, which allosterically regulates Cav2.2 to achieve analgesia and pain relief without negative side effect profiles. |
| TTA-A8
TTA-A8 is a short-acting T-type calcium channel antagonist with oral activity, exhibiting an IC50 value of 31.3 nM in the FLIPR depolarization assay. |
| MONIRO-1
MONIRO-1 is a T-type and N-type calcium channel blocker with IC50 values of 34, 3.3, 1.7 and 7.2 µM against hCav2.2, hCav3.1, hCav3.2 and hCav3.3, respectively. |
| Azumolene
Azumolene (EU4093 free base), a Dantrolene analog, is a muscle relaxant. |
| Nexopamil
Nexopamil is a calcium antagonist of Ca2+ channel, 5HT2, 5HT1A, 5HT1C and dopamine D2 receptors. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
