Oxcarbazepine Inhibitor CAS No. 28721-07-5

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KI1365	Oxcarbazepine	10 mg	$154
KI1365	Oxcarbazepine	50 mg	$496

Chemical Characteristic

Product Name	Oxcarbazepine
Synonyms	Trileptal
CAS No.	28721-07-5
Molecular Weight	252.26
Formula	C₁₅H₁₂N₂O₂
Chemical Name	10,11-Dihydro-10-oxo-5H-dibenz[b,f]azepine-5-carboxamide
Smiles	N1(c2c(CC(=O)c3c1cccc3)cccc2)C(=O)N
Chemical Structure

Biological activities

Oxcarbazepine is an anticonvulsant and mood stabilizing drug. Oxcarbazepine is used primarily in the treatment of not only epilepsy but also anxiety and mood disorders. Oxcarbazepine blocks the frequency of firing of sodium-dependent action potentials by cultured mouse central neurons with IC50 of 50 nM.^[1] Oxcarbazepine reduces L-type calcium currents by about 30% at the concentration of 0.3 mM. ^[2] Oxcarbazepine generates a marked concentration- and frequency-dependent reduction in the compound action potential amplitude.^[3] Oxcarbazepine (0.3-30 µM) induces a reversible reduction in the amplitude of voltage-gated Na⁺ current (INa) with an IC50 of 3.1 µM.^[4] Oxcarbazepine treats generalized tonic-clonic seizures induced by electroshock in mice and rats with ED50 values ranging from 13.5 to 20.5 mg/kg p.o. Oxcarbazepine does not produce tolerance toward this anticonvulsant effect in the process of 4-week treatment. ^[2] Intravenous administration of oxcarbazepine (1-10 mg/kg) inhibits the P3 component in a dose-dependent manner.^[5]

Protocols

Oxcarbazepine is dissolved in PEG400 in vivo assay.^[5]

References

[1] McLean MJ, et al. Oxcarbazepine: Mechanisms of Action. Epilepsia. 1994, 35 Suppl 3: S5-S9. [2] Schmutz M, et al. Oxcarbazepine: preclinical anticonvulsant profile and putative mechanisms of action. Epilepsia. 1994, 35 Suppl 5: S47-S50. [3] Guven M, et al. The conduction block produced by oxcarbazepine in the isolated rat sciatic nerve: a comparison with lamotrigine. Neurol Res. 2011, 33(1): 68-74. [4] Huang CW, et al. The synergistic inhibitory actions of oxcarbazepine on voltage-gated sodium and potassium currents in differentiated NG108-15 neuronal cells and model neurons. Int J Neuropsychopharmacol. 2008, 11(5): 597-610. [5] Kiguchi S, et al. Suppressive effects of oxcarbazepine on tooth pulp-evoked potentials recorded at the trigeminal spinal tract nucleus in cats. Clin Exp Pharmacol Physiol. 2001, 28(3): 169-175.

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