Prenylamine block of Nav1.5 channel is mediated via a receptor distinct from that of local anesthetics.

@article{Mujtaba2002PrenylamineBO,
  title={Prenylamine block of Nav1.5 channel is mediated via a receptor distinct from that of local anesthetics.},
  author={M. Mujtaba and Sho-Ya Wang and G. Wang},
  journal={Molecular pharmacology},
  year={2002},
  volume={62 2},
  pages={
          415-22
        }
}
We have shown previously that prenylamine, a calcium channel blocker, has potent local anesthetic activity in vivo and in vitro. We now characterize the tonic and use-dependent block of prenylamine on wild-type human cardiac voltage-gated sodium channels (hNav1.5) transiently expressed in human embryonic kidney 293t cells under whole-cell voltage-clamp condition. We also determine whether prenylamine and local anesthetics interact with a common binding site on the Nav1.5 channel by analyzing… Expand
Nav1.5 Voltage-Gated Sodium Channel
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References

SHOWING 1-10 OF 26 REFERENCES
Local Anesthetic Properties of Prenylamine
Distinct local anesthetic affinities in Na+ channel subtypes.
Local anesthetics: hydrophilic and hydrophobic pathways for the drug- receptor reaction
  • B. Hille
  • Medicine, Chemistry
  • The Journal of general physiology
  • 1977
Residues in Na(+) channel D3-S6 segment modulate both batrachotoxin and local anesthetic affinities.
Disparate role of Na(+) channel D2-S6 residues in batrachotoxin and local anesthetic action.
Block of Human Heart hH1 Sodium Channels by the Enantiomers of Bupivacaine
State-dependent cocaine block of sodium channel isoforms, chimeras, and channels coexpressed with the beta1 subunit.
From Ionic Currents to Molecular Mechanisms The Structure and Function of Voltage-Gated Sodium Channels
...
1
2
3
...