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Carbamazepine is a sodium channel inhibitor with an IC50 of 131 μM when treated with synaptosomes in rat brain. Carbamazepine blocks voltage gated Na+, Ca2+, and K+ channels, and is also a HDAC inhibitor (IC50=2 μM). Voltage-gated sodium channels are the molecular pores that allow brain cells (neurons) to generate action potentials, the electrical events that allow neurons to communicate over long distances. After the sodium channels open to start the action potential, they inactivate, essentially closing the channel. Carbamazepine stabilizes the inactivated state of sodium channels, meaning that fewer of these channels are available to subsequently open, making brain cells less excitable.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Male Wistar rats |
| Formulation | Dissolved in saline/DMSO (50/50 vol/vol) |
| Dosages | ~100 mg/kg |
| Administration | Injected intraperitoneally (i.p.) |
| Molecular Weight | 236.27 |
| Formula | C15H12N2O |
| CAS Number | 298-46-4 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[7] R H Levy, et al. Clinical pharmacokinetics of carbamazepine
| Related Sodium Channel Products |
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Rilutek is a sodium channel protein inhibitor and a new mental compound, which has anticonvulsant, hypnotic, antianxiety, antiischemia and anesthesia properties. Riluzole belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM. |
| A-803467
A-803467 is a potent and selective Nav1.8 sodium channel blocker that potently blocks tetrodotoxin-resistant currents (IC50 = 140 nM). |
| Oxcarbazepine
Oxcarbazepine is an anticonvulsant and mood-stabilizing compound. |
| Ambroxol hydrochloride
AmbroxolHCl is a potent inhibitor of the neuronal Na+ channels, inhibits TTX-resistant Na+ currents with IC50 of 35.2 μM and 22.5 μM for tonic and phasic block, inhibits TTX-sensitive Na+ currents with IC50 of 100 μM. |
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