Local anesthetic block of Kv channels: role of the S6 helix and the S5-S6 linker for bupivacaine action.

@article{Nilsson2003LocalAB,
  title={Local anesthetic block of Kv channels: role of the S6 helix and the S5-S6 linker for bupivacaine action.},
  author={Johanna Nilsson and M. Gregor Madeja and Peter {\AA}rhem},
  journal={Molecular pharmacology},
  year={2003},
  volume={63 6},
  pages={
          1417-29
        }
}
To gain insights in the molecular mechanisms of anesthesia, we analyzed the effects of bupivacaine on a series of voltage-gated K+ channels (Kv1.1, -1.2, -1.5, -2.1, -3.1, and -3.2) and various mutant channels derived from Kv2.1, using Xenopus laevis oocytes. Two phenomenologically different blocking effects were seen at room temperature: a time-dependent block of Kv1 and Kv3 channels (Kd between 110 and 240 microM), and a time-independent block on Kv2.1 (Kd = 220 microM). At 32 degrees C… CONTINUE READING

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Principles of Physical Chemistry with Applications to the Biological Sciences

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