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An Activator of NaV Channels

Cat #: A-150
Alternative Name Acetylbenzoylaconine
Lyophilized Powder yes
  • Bioassay Tested
  • Origin Aconitum karacolium.
    Source Natural
    MW: 645.74
    Purity: >98% (HPLC)
    Effective concentration 100 nM - 1 μM.
    Chemical name (1α,3α,6α,14α,15α,16β)-20-Ethyl-1,6,16-trimethoxy-4-(methoxymethyl)aconitane-3,8,13,14,15-pentol 8-acetate 14-benzoate.
    Molecular formula C34H47NO11.
    CAS No.: 302-27-2
    Activity Aconitine modulates voltage-dependent sodium channels in a complex way1. It activates the channel at low voltages, while at high voltages its effects appear inhibitory.
    1. Rao, S. and Sikdar, S.K. (2000) Pflügers Arch439, 349.
    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, ethanol. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs Aconitine modulates native TTX-sensitive NaV channel currents in ND7/23 cells.
      Alomone Labs Aconitine modulates native TTX-sensitive NaV channel currents in ND7/23 cells.
      NaV currents were elicited by a 50 ms voltage ramp from the holding potential of -100 mV to +60 mV, applied every 10 sec using whole-cell voltage clamp. A. Time course of current at -20 mV (black) and -30 mV (green) along the voltage ramp, showing the effect of 0.8 μM Aconitine (#A-150) application (horizontal bar) on current voltage dependence. B. Superimposed traces of NaV currents in ND7/23 cells under control conditions and after 6 min perfusion with 0.8 μM Aconitine (as indicated).
    References - Scientific background
    1. Wright, S.N. (2002) J. Physiol. 538, 759.
    2. Cestele, S. and Catterall, W.A. (2000) Biochimie 82, 883.
    3. Ameri A. (1998) Prog. Neurobiol. 56, 211.
    4. Mizugaki, M. et al. (1998) J. Anal. Toxicol. 22, 336.
    5. Zhang. L. et al. (2007) J. Sep. Sci. 30, 1357.
    6. Ulbricht, W. (1998) Rev. Physiol. Biochem. Pharmacol. 133, 1.
    7. Suzuki, Y. et al. (1994) Planta Med. 60, 391.
    Scientific background

    Voltage-gated sodium channels (NaV) are pres­ent in most excitable cell membranes and play an important role in generating action potentials. A variety of toxins and chemi­cals are known to either block or modu­late Na+ channels and have proven to be invaluable in investigating the physiological characteristics of these channels1. Most notably, tetrodotoxin (TTX), a potent and selective blocker of Na+ channels, binds to neurotoxin receptor site 1 to block them2.

    Aconitine is a diterpense two-ester alkaloid derived from the tubers of aconitinum plants and has been used as traditional herbal medicine in China and Japan since ancient times. Modern pharmacological studies have shown that aconitine has effects of analgesia and anesthesia, anti-inflammatory, immune regulation, anti-tumor and cardiotonic actions3,4. Concurrently, aconitine also presents enormous toxicity5. It is well known for its toxic effects on the heart and central nervous system where it causes cardiac arrhythmias, systemic paralysis and coma6. Aconitine alters the kinetics and voltage dependence of Na+ chan­nel activation, inhibits Na+ channel inactivation through binding to neurotoxin receptor site 2 and causes persistent activation of Na+ channels at the resting mem­brane potential7.

    Target NaV Na+ channels
    Last update: 06/11/2022

    Aconitine (#A-150) is a highly pure, natural, and biologically active compound.

    For research purposes only, not for human use



    Product citations
    1. Ferreira, F. et al. (2016) Development 143, 4582.


    Scientific Background

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