Inactivation gating determines drug potency: a common mechanism for drug blockade of HERG channels.

@article{Yang2004InactivationGD,
  title={Inactivation gating determines drug potency: a common mechanism for drug blockade of HERG channels.},
  author={Baofeng Yang and Dong-hui Xu and Chao-qian Xu and Zhe Li and Zhi-min Du and Hui-zhen Wang and De-Li Dong},
  journal={Acta pharmacologica Sinica},
  year={2004},
  volume={25 5},
  pages={554-60}
}
AIM To determine the mechanisms of interactions between different drugs and HERG channels. METHODS Various antiarrhythmic (dofetilide, quinidine, azimilide, RP58866) and non-antiarrhythmic (terfenadine, nicotine) agents were used on HERG channels expressed in Xenopus oocyte. Whole-cell voltage-clamp techniques were used. RESULTS All drugs produced concentration-dependent block of HERG current. The inhibition was markedly facilitated with voltage protocols favoring channel inactivation (eg… CONTINUE READING