A new negative allosteric modulator, AP14145, for the study of small conductance calcium-activated potassium (KCa 2) channels.

@article{SimVicens2017ANN,
  title={A new negative allosteric modulator, AP14145, for the study of small conductance calcium-activated potassium (KCa 2) channels.},
  author={Rafel Sim{\'o}-Vicens and Jeppe Egedal Kirchhoff and Bernardo Dolce and Lea Abildgaard and Tobias Speerschneider and Ulrik S S{\o}rensen and Morten Grunnet and Jonas G Diness and Bo Hjorth Bentzen},
  journal={British journal of pharmacology},
  year={2017},
  volume={174 23},
  pages={
          4396-4408
        }
}
BACKGROUND AND PURPOSE Small conductance calcium-activated potassium (KCa 2) channels represent a promising atrial-selective target for treatment of atrial fibrillation. Here, we establish the mechanism of KCa 2 channel inhibition by the new compound AP14145. EXPERIMENTAL APPROACH Using site-directed mutagenesis, binding determinants for AP14145 inhibition were explored. AP14145 selectivity and mechanism of action were investigated by patch-clamp recordings of heterologously expressed KCa 2… CONTINUE READING
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