Blocker State Dependence and Trapping in Hyperpolarization-Activated Cation Channels

  title={Blocker State Dependence and Trapping in Hyperpolarization-Activated Cation Channels},
  author={Ki Soon Shin and Brad S Rothberg and Gary Yellen},
  journal={The Journal of General Physiology},
  pages={91 - 102}
Hyperpolarization-activated cation currents (I(h)) are key determinants of repetitive electrical activity in heart and nerve cells. The bradycardic agent ZD7288 is a selective blocker of these currents. We studied the mechanism for ZD7288 blockade of cloned I(h) channels in excised inside-out patches. ZD7288 blockade of the mammalian mHCN1 channel appeared to require opening of the channel, but strong hyperpolarization disfavored blockade. The steepness of this voltage-dependent effect (an… CONTINUE READING


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