A small molecule activator of Nav 1.1 channels increases fast-spiking interneuron excitability and GABAergic transmission in vitro and has anti-convulsive effects in vivo.

@article{Frederiksen2017ASM,
  title={A small molecule activator of Nav 1.1 channels increases fast-spiking interneuron excitability and GABAergic transmission in vitro and has anti-convulsive effects in vivo.},
  author={Kristen Frederiksen and Dunguo Lu and Jinhui Yang and Henrik Sindal Jensen and Jesper Frank Bastlund and Peter Hj\orringgaard Larsen and Henry Liu and François Crestey and Kim Dekermendjian and Lassina Badolo and Morten Laursen and Charlotte O Hougaard and Charles R. Yang and Niels Svenstrup and Morten Grunnet},
  journal={The European journal of neuroscience},
  year={2017},
  volume={46 3},
  pages={
          1887-1896
        }
}
Nav 1.1 (SCN1A) channels primarily located in gamma-aminobutyric acid (GABA)ergic fast-spiking interneurons are pivotal for action potential generation and propagation in these neurons. Inappropriate function of fast-spiking interneurons, leading to disinhibition of pyramidal cells and network desynchronization, correlates with decreased cognitive capability. Further, reduced functionality of Nav 1.1 channels is linked to various diseases in the central nervous system. There is, at present… CONTINUE READING