Bis-tetrahydroisoquinoline derivatives: AG525E1, a new step in the search for non-quaternary non-peptidic small conductance Ca(2+)-activated K(+) channel blockers.

@article{Graulich2008BistetrahydroisoquinolineDA,
  title={Bis-tetrahydroisoquinoline derivatives: AG525E1, a new step in the search for non-quaternary non-peptidic small conductance Ca(2+)-activated K(+) channel blockers.},
  author={Amaury Graulich and C{\'e}dric Lamy and Livia Alleva and S{\'e}bastien Dilly and Philippe Chavatte and Johan Wouters and Vincent Seutin and Jean-François Li{\'e}geois},
  journal={Bioorganic & medicinal chemistry letters},
  year={2008},
  volume={18 11},
  pages={3440-5}
}
So far, small conductance Ca(2+)-activated K(+) channel (SK) blockers mostly consist of quaternary ammonium derivatives or peptides. Due to their physicochemical properties, these blockers are not suitable to study the physiological roles of SK channels in the central nervous system in vivo. Herein, we report the discovery of a chiral bis-tertiary amine… CONTINUE READING