Oxcarbazepine

OXC, Trileptal®, Timox®
A Use-Dependent Anti-Epileptic NaV Channel Blocker
    Cat #: O-105
    Alternative Name OXC, Trileptal®, Timox®
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 252.3
    Purity: >98%
    Effective concentration 20 nM - 200 µM.
      • Oxcarbazepine
    Chemical name 10,11-Dihydro-10-oxo-5H-dibenzo(Z)[b,f]azepine-5-carboxamide.
    Molecular formula C15H12N2O2.
    CAS No.: 28721-07-5.
    Activity Oxcarbazepine is an anticonvulsant drug. Its main mechanism of action is the inhibition of voltage-dependent Na+ channels1. Oxcarbazepine (IC50 = 50 nM) and its rapidly formed monohydroxy metabolite, MHD, (IC50 = 20 nM) inhibit sustained, high frequency, repetitive action potential firing of cultured spinal cord neurons2.
      • Ambrosio, A. F. et al. (2002) Neurochem. Res. 27, 121.
      • McLean, M. J. et al. (1994) Epilepsia 35, S55.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to one week at 4°C or three months at -20°C.
      • Oxcarbazepine
        Alomone Labs Oxcarbazepine inhibits NaV1.7 channels currents in HEK293 cells.
        A.Time course of current reversible inhibition by 200 μM Oxcarbazepine (#O-105). Currents were elicited by a voltage ramp from a holding potential of -100 mV to 60 mV (30 ms) delivered every 10 seconds. B. Example traces of current response to voltage ramp stimulation before and during 200 μM Oxcarbazepine application.
    References - Scientific background
    • 1. Ambrosio, A. F. et al. (2002) Neurochem. Res. 27, 121.
    • 2. Rogawski, M. A. et al. (1990) Pharmacol. Rev. 42, 223.
    • 3. Wolfe, J.F. et al. (1998) Exp. Opin. Ther. Patents 8, 361.
    • 4. Reinikainen, K. J. et al. (1987) Epilepsy Res. 1, 284.
    • 5. Koch, M. W. et al. (2009) Cochrane Database Sys. Rev. CD006453.
    • 6. McLean, M. J. et al. (1994) Epilepsia 35, S55.
    • 7. Wamil, A. W. et al. (1991) Epilepsia 32, 65.
    • 8. Wamil, A. W. et al. (1994) Eur. J. Pharmacol. 271, 301.
    • 9. Schmutz, M. et al. (1994) Epilepsia 35, S47.
    • 10. Benes, J. W. et al. (1999) J. Med. Chem. 42, 2582.
      • Epilepsy is one of the most common neurological disorders and it is estimated that the majority of epileptic patients are treated with only four drugs: phenobarbital, phenytoin, carbamazepine (CBZ) and valproic acid. It is widely accepted that the majority of antiepileptic drugs (AEDs) act by more than one mechanism1.

        Oxcarbazepine (OCBZ) is an anticonvulsant drug and its main mechanism of action is the inhibition of voltage-dependent Na+ channels1.

        OCBZ is a keto homologue of CBZ with a completely different metabolic profile. OCBZ and CBZ have a comparable anticonvulsant efficacy, but OCBZ has the advantage of a low incidence of allergic reactions, enzyme induction and side effects2,3.

        Clinical trials, with OCBZ treated patients with epilepsy, confirmed the efficacy, tolerability, and safety of OCBZ at a daily dose of 30–46 mg/kg (600–2400 mg/day) as a first-line treatment for children, adolescents, and adults with partial seizures including simple partial seizures, complex partial seizures, and secondarily generalized seizures4,5.

        In humans, the keto group of OCBZ is rapidly and quantitatively reduced to form a monohydroxy derivative (MHD), which is the main active agent during OCBZ therapy. OCBZ (IC50 - 500 µM) and MHD (IC50 - 200 µM)6 inhibit sustained, high frequency, repetitive firing of cultured spinal cord neurons due to an inhibitory effect on voltage-dependent sodium channels. This effect was found to be voltage- and frequency-dependent6-9. Neurochemical studies also showed that OCBZ binds to sodium channels and modulates sodium entry in cortical synaptosomes10. An additional mechanism of action such as an effect on potassium channels, might be also clinically important6.

    Target TTX-Sensitive NaV channels
    Last update: 24/01/2020

    Oxcarbazepine (#O-105) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use