Local anesthetics: hydrophilic and hydrophobic pathways for the drug- receptor reaction

@article{Hille1977LocalAH,
  title={Local anesthetics: hydrophilic and hydrophobic pathways for the drug- receptor reaction},
  author={Bertil Hille},
  journal={The Journal of General Physiology},
  year={1977},
  volume={69},
  pages={497 - 515}
}
The properties of Na channels of the node of Ranvier are altered by neutral, amine, and quaternary local anesthetic compounds. The kinetics of the Na currents are governed by a composite of voltage- and time-dependent gating processes with voltage- and time-dependent block of channels by drug. Conventional measurements of steady-state sodium inactivation by use of 50-ms prepulses show a large negative voltage shift of the inactivation curve with neutral benzocaine and with some ionizable amines… CONTINUE READING

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