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Related Experiment Videos

Interaction between batrachotoxin and yohimbine.

L Y Huang, G Ehrenstein, W A Catterall

    Biophysical Journal
    |August 1, 1978
    PubMed
    Summary
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    Yohimbine, an alkaloid, competitively inhibits batrachotoxin-activated sodium channel activity in neuroblastoma cells. This neurotoxin research reveals yohimbine affects channel gating, not channel blockage.

    Area of Science:

    • Neuroscience
    • Pharmacology
    • Molecular Biology

    Background:

    • Specific activators of sodium channels, batrachotoxin and veratridine, increase sodium uptake in neuroblastoma cells.
    • Yohimbine, an indolakylamine alkaloid, has been observed to inhibit batrachotoxin-induced sodium uptake.

    Purpose of the Study:

    • To investigate the inhibitory mechanism of yohimbine on batrachotoxin-activated sodium channels.
    • To determine the binding characteristics and mode of inhibition of yohimbine.

    Main Methods:

    • Utilized neuroblastoma cells to measure 22Na uptake.
    • Administered batrachotoxin and yohimbine to assess their effects on sodium flux.
    • Performed dose-response, kinetic, and equilibrium binding experiments.
    • Varied membrane potential to evaluate the effect on yohimbine's dissociation constant.

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    Main Results:

    • Yohimbine competitively inhibits batrachotoxin-induced 22Na uptake.
    • The inhibition by yohimbine involves a single class of reversible binding sites with a dissociation constant of 3-4 x 10(-5) M.
    • The dissociation constant of yohimbine was unaffected by changes in membrane depolarization.
    • Yohimbine acts on the channel gating mechanism rather than occluding the channel.

    Conclusions:

    • Yohimbine is a competitive inhibitor of batrachotoxin's action on sodium channels.
    • The findings suggest yohimbine modulates sodium channel function by altering the gating mechanism.
    • This study provides insight into the interaction of alkaloids with voltage-gated sodium channels.