Potent blockade of sodium channels and protection of brain tissue from ischemia by BIII 890 CL.

@article{Carter2000PotentBO,
  title={Potent blockade of sodium channels and protection of brain tissue from ischemia by BIII 890 CL.},
  author={A. J. Carter and Matthias Grauert and Uwe Pschorn and Wolf Dietrich Dr Bechtel and C. Bartmann-Lindholm and Yusheng Qu and Todd Scheuer and W. A. Catterall and Thomas Weiser},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  year={2000},
  volume={97 9},
  pages={
          4944-9
        }
}
  • A. J. Carter, M. Grauert, T. Weiser
  • Published 25 April 2000
  • Biology, Chemistry
  • Proceedings of the National Academy of Sciences of the United States of America
We have synthesized a new benzomorphan derivative, 2R-[2alpha,3(S*), 6alpha]-1,2,3,4,5,6-hexahydro-6,11, 11-trimethyl-3-[2-(phenylmethoxy)propyl]-2, 6-methano-3-benzazocin-10-ol hydrochloride (BIII 890 CL), which displaced [(3)H]batrachotoxinin A-20alpha-benzoate from neurotoxin receptor site 2 of the Na(+) channel in rat brain synaptosomes (IC(50) = 49 nM), but exhibited only low affinity for 65 other receptors and ion channels. BIII 890 CL inhibited Na(+) channels in cells transfected with… 

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