Electrostatic contributions of aromatic residues in the local anesthetic receptor of voltage-gated sodium channels.

@article{Ahern2008ElectrostaticCO,
  title={Electrostatic contributions of aromatic residues in the local anesthetic receptor of voltage-gated sodium channels.},
  author={Christopher A. Ahern and Amy L. Eastwood and Dennis A Dougherty and Richard Horn},
  journal={Circulation research},
  year={2008},
  volume={102 1},
  pages={86-94}
}
Antiarrhythmics, anticonvulsants, and local anesthetics target voltage-gated sodium channels, decreasing excitability of nerve and muscle cells. Channel inhibition by members of this family of cationic, hydrophobic drugs relies on the presence of highly conserved aromatic residues in the pore-lining S6 segment of the fourth homologous domain of the channel. We tested whether channel inhibition was facilitated by an electrostatic attraction between lidocaine and pi electrons of the aromatic… CONTINUE READING

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