Mechanisms of use-dependent block of sodium channels in excitable membranes by local anesthetics.

@article{Starmer1984MechanismsOU,
  title={Mechanisms of use-dependent block of sodium channels in excitable membranes by local anesthetics.},
  author={C. Frank Starmer and Augustus O. Grant and Harold C. Strauss},
  journal={Biophysical journal},
  year={1984},
  volume={46 1},
  pages={15-27}
}
Many local anesthetics promote reduction in sodium current during repetitive stimulation of excitable membranes. Use-, frequency-, and voltage-dependent responses describe patterns of peak INa when pulse width, pulse frequency, and pulse amplitude are varied. Such responses can be viewed as reflecting voltage-sensitive shifts in equilibrium between conducting, unblocked channels and nonconducting, blocked channels. The modulated-receptor hypothesis postulates shifts in equilibrium as the result… CONTINUE READING

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