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Carbamazepine

CBZ, Tegretol®
A State-Dependent NaV Channel Blocker
Cat #: C-105
Alternative Name CBZ, Tegretol®
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 236.3
    Purity: >99%
    Effective concentration IC50 ~ 1 mM.
    Structure
    Chemical name 5H-Dibenz[b,f]azepine-5-carboxamide.
    Molecular formula C15H12N2O.
    CAS No.: 298-46-4.
    Activity Carbamazepine is a potent and state-dependent blocker of neuronal NaV channels1. It is one of the most commonly prescribed antiepileptic drugs2 and has long been established as a treatment for neuropathic pain3.
    References-Activity
    1. Sheets, P.L. et al. (2008) J. Pharmacol. Exp. Ther. 326, 89.
    2. Kuo, C.C. et al. (1997) Mol. Pharmacol. 51, 1077.
    3. Backonja, M.M. (2002) Neurology 59, S14.
    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.
    Our bioassay
    • Alomone Labs Carbamazepine inhibits NaV1.2 channels currents in Xenopus oocytes.
      Alomone Labs Carbamazepine inhibits NaV1.2 channels currents in Xenopus oocytes.
      A. Time course of NaV1.2 channel reversible inhibition by 100 µM and 1 mM Carbamazepine (#C-105). Currents were elicited by a voltage step to -20 mV (100 ms) every 10 seconds from a holding potential of -100 mV.  B. Example traces of current response to voltage step application before and during 1 mM Carbamazepine application.
    References - Scientific background
    1. Sheets, P.L. et al. (2008) J. Pharmacol. Exp. Ther. 326, 89.
    2. Zimmermann, K. et al. (2007) Nature 447, 855.
    3. Kuo, C.C. et al. (1997) Mol. Pharmacol. 51, 1077.
    4. Backonja, M.M. (2002) Neurology 59, S14.
    5. Fertleman, C.R. et al. (2006) Neuron 52, 767.
    6. Fertleman, C.R. et al. (2007) Neurology 69, 586.
    7. Calabresi, P. et al. (2007) Trends. Pharmacol. Sci. 28, 188.
    Scientific background

    Voltage-gated sodium channels (VGSC, NaV) play a critical role in excitability of nociceptors (pain-sensing neurons). The peripheral-specific sodium channels NaV1.7, NaV1.8 and NaV1.9 are particularly important in the pathophysiology of different pain syndromes and hence, thought to be potential targets for pain therapeutics1,2.

    Carbamazepine is a potent and state dependent inhibitor of neuronal NaV channels1. It is one of the most commonly prescribed antiepileptic drugs3 and has long been established as a treatment for neuropathic pain4. High doses of carbamazepine are effective in ameliorating symptoms of patients with Paroxysmal extreme pain disorder (PEPD) because this disorder involves changes in NaV inactivation, a process that is modulated by NaV blockers. In a recent investigation, patients with inherited erythromelalgia, characterized by a mutation in NaV1.7 (SCN9A) and a modified fast inactivation of Na+ current is present, reported an improvement of symptoms when treated with Carbamazepine5,6. In addition, clinical data also suggest that carbamazepine can reduce aura and migraine attacks7.

    Target NaV channels
    Last update: 22/09/2020

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

    For research purposes only, not for human use
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