Lomerizine dihydrochloride is a relatively new L- and T-type calcium channel blocker used in the treatment of migraine.
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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 |
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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 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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