The Investigational Anticonvulsant Lacosamide Selectively Enhances Slow Inactivation of Voltage-Gated Sodium Channels

@article{Errington2008TheIA,
  title={The Investigational Anticonvulsant Lacosamide Selectively Enhances Slow Inactivation of Voltage-Gated Sodium Channels},
  author={Adam C. Errington and Thomas St{\"o}hr and Cara Heers and George Lees},
  journal={Molecular Pharmacology},
  year={2008},
  volume={73},
  pages={157 - 169}
}
We hypothesized that lacosamide modulates voltage-gated sodium channels (VGSCs) at clinical concentrations (32-100 μM). Lacosamide reduced spiking evoked in cultured rat cortical neurons by 30-s depolarizing ramps but not by 1-s ramps. Carbamazepine and phenytoin reduced spike-firing induced by both ramps. Lacosamide inhibited sustained repetitive firing during a 10-s burst but not within the first second. Tetrodotoxin-sensitive VGSC currents in N1E-115 cells were reduced by 100 μM lacosamide… 
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  • S. Jo, B. Bean
  • Chemistry, Medicine
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TLDR
Results show that BBG inhibits voltage-gated sodium channels at micromolar concentrations, and suggest there may be significant inhibition of sodium channels in spinal cord or brain during experimental treatment of spinal cord injury or Huntington's disease.
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