Unexpected mexiletine responses of a mutant cardiac Na+ channel implicate the selectivity filter as a structural determinant of antiarrhythmic drug access.

@article{Sasaki2004UnexpectedMR,
  title={Unexpected mexiletine responses of a mutant cardiac Na+ channel implicate the selectivity filter as a structural determinant of antiarrhythmic drug access.},
  author={Koji Sasaki and Naomasa Makita and Akihiko Sunami and Harumizu Sakurada and Nobumasa Shirai and Hisataka Yokoi and Akinori Kimura and Noritsugu Tohse and Masayasu Hiraoka and Akira Kitabatake},
  journal={Molecular pharmacology},
  year={2004},
  volume={66 2},
  pages={330-6}
}
Gating properties of Na(+) channels are the critical determinants for the state-dependent block by class I antiarrhythmic drugs; however, recent site-directed mutagenesis studies have shown that the Na(+) channel selectivity filter region controls drug access to and dissociation from the binding site. To validate these observations, we have exploited a naturally occurring cardiac Na(+) channel mutation, S1710L, located next to the putative selectivity filter residue of domain 4, and evaluated… CONTINUE READING

Citations

Publications citing this paper.
Showing 1-10 of 10 extracted citations

References

Publications referenced by this paper.
Showing 1-10 of 30 references

Ion Channels of Excitable Membranes

  • B Hille
  • 3rd ed. Sinauer Associates,
  • 2001
2 Excerpts

Similar Papers

Loading similar papers…