Molecular mechanisms of K+ channel blockade: 4-aminopyridine interaction with a cloned cardiac transient K+ (Kv1.4) channel

Adv Exp Med Biol. 1995:382:11-22. doi: 10.1007/978-1-4615-1893-8_2.

Abstract

We studied the blocking effects of 4-aminopyridine (4-AP) on a Kv1.4 K+ channel. A permanently charged 4-AP derivative only produced block when applied intracellularly. 4-AP block accumulated from pulse to pulse indicating trapping of 4-AP in deactivated channels. For long trains of depolarizing pulses, 4-AP block increased with decreasing pulse duration. This increase took many pulses (> 10) to accumulate and was relieved by two to three subsequent pulses of 500 msec duration. We conclude that the time- and voltage-dependence of 4-AP block can not be accounted for solely by either simple pure open channel or pure closed channel blocking schemes. We propose that the data can be explained by a model in which 4-AP binding is most stable when the channel has a symmetric arrangement in the binding regions.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • 4-Aminopyridine / pharmacology*
  • Animals
  • DNA, Complementary / genetics
  • DNA, Complementary / isolation & purification
  • Electrophysiology
  • Ferrets
  • Ion Channel Gating / drug effects*
  • Myocardium / metabolism*
  • Potassium Channel Blockers*
  • Potassium Channels / genetics
  • Xenopus laevis

Substances

  • DNA, Complementary
  • Potassium Channel Blockers
  • Potassium Channels
  • 4-Aminopyridine