Carbamazepine (Carbatrol) is a sodium channel blocker with an IC50 of 140 uM. 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.
|Animal models||Male Wistar rats|
|Formulation||Dissolved in saline/DMSO (50/50 vol/vol)|
|Administration||Injected intraperitoneally (i.p.)|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 40 mg/mL|
|Related Sodium Channel Products|
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Eleclazine HCl is a novel late Na+ current inhibitor, with IC50 value of 0.7 uM.
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