Mechanism of block and identification of the verapamil binding domain to HERG potassium channels.

@article{Zhang1999MechanismOB,
  title={Mechanism of block and identification of the verapamil binding domain to HERG potassium channels.},
  author={Song-fu Zhang and Zhengfeng Zhou and Qiying Gong and Jonathan C. Makielski and Craig T. January},
  journal={Circulation research},
  year={1999},
  volume={84 9},
  pages={989-98}
}
Calcium channel antagonists have diverse effects on cardiac electrophysiology. We studied the effects of verapamil, diltiazem, and nifedipine on HERG K+ channels that encode IKr in native heart cells. In our experiments, verapamil caused high-affinity block of HERG current (IC50=143.0 nmol/L), a value close to those reported for verapamil block of L-type Ca2+ channels, whereas diltiazem weakly blocked HERG current (IC50=17.3 micromol/L), and nifedipine did not block HERG current. Verapamil… CONTINUE READING

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