Molecular dissection of lubeluzole use-dependent block of voltage-gated sodium channels discloses new therapeutic potentials.

@article{Desaphy2013MolecularDO,
  title={Molecular dissection of lubeluzole use-dependent block of voltage-gated sodium channels discloses new therapeutic potentials.},
  author={Jean-François Desaphy and Roberta Carbonara and Teresa Costanza and Giovanni Lentini and Maria Maddalena Cavalluzzi and Claudio Bruno and Carlo Franchini and Diana Conte Camerino},
  journal={Molecular pharmacology},
  year={2013},
  volume={83 2},
  pages={406-15}
}
Lubeluzole, which acts on various targets in vitro, including voltage-gated sodium channels, was initially proposed as a neuroprotectant. The lubeluzole structure contains a benzothiazole moiety [N-methyl-1,3-benzothiazole-2-amine (R-like)] related to riluzole and a phenoxy-propranol-amine moiety [(RS)-1-(3,4-difluorophenoxy)-3-(piperidin-1-yl)propan-2-ol (A-core)] recalling propranolol. Both riluzole and propranolol are efficient sodium channel blockers. We studied in detail the effects of… CONTINUE READING