Relationship between structure and sodium channel blockade by lidocaine and its amino-alkyl derivatives.

@article{Liu1994RelationshipBS,
  title={Relationship between structure and sodium channel blockade by lidocaine and its amino-alkyl derivatives.},
  author={Lieju Liu and David J. Wendt and Augustus O. Grant},
  journal={Journal of cardiovascular pharmacology},
  year={1994},
  volume={24 5},
  pages={803-12}
}
We examined the relationship between the physicochemical properties and the sodium channel-blocking actions of lidocaine and four of its amino-alkyl derivatives. The homologues differ in lipid solubility (log p 2.7-4.1), pKa (6.9-9.0), and molecular weight (248.5-290.7). Macroscopic sodium currents were measured in rabbit atrial myocytes by the whole-cell configuration of patch-clamp technique; single-channel currents were measured by the cell-attached configuration. Lidocaine and its… CONTINUE READING