Barium block of the muscarinic potassium current in guinea-pig atrial cells

Pflugers Arch. 1995 Jul;430(3):348-57. doi: 10.1007/BF00373909.

Abstract

Block of the muscarinic K+ current (iK,ACh) by Ba2+ has been studied in guinea-pig atrial cells using the whole-cell patch-clamp technique. The dose-response curve for the block of iK,ACh can be fitted assuming that a muscarinic K+ channel is blocked when a single Ba2+ ion binds to it (apparent dissociation constant, Kd = 125 microM at 0 mV). Block was voltage and time dependent. The voltage dependence can be explained by Ba2+ binding to a site within the pore of the channel, 36% across the width of the membrane electric field (from the outside). Raising the bathing K+ concentration reduced Ba2+ block of iK,ACh, which suggests that Ba2+ and K+ compete for a common binding site. When Ba2+ was added during an exposure to ACh (muscarinic K+ channel open), block of iK,ACh developed rapidly, but when Ba2+ was added prior to an exposure to ACh (muscarinic K+ channel closed), little block of iK,ACh was evident when ACh was first applied. This suggests that when the muscarinic K+ channel is closed in the absence of ACh, Ba2+ does not have access to the binding site within the pore of the channel. In conclusion, Ba2+ block of iK,ACh is concentration, voltage, time, K+ and state dependent.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Barium / pharmacology*
  • Binding Sites / drug effects
  • Electrophysiology
  • Guinea Pigs
  • Heart Atria / cytology
  • Heart Atria / drug effects
  • Heart Atria / metabolism
  • In Vitro Techniques
  • Membrane Potentials / drug effects
  • Muscarinic Antagonists / pharmacology*
  • Myocardium / metabolism*
  • Patch-Clamp Techniques
  • Potassium / metabolism
  • Potassium Channels / drug effects
  • Potassium Channels / metabolism*
  • Receptors, Muscarinic / metabolism*

Substances

  • Muscarinic Antagonists
  • Potassium Channels
  • Receptors, Muscarinic
  • Barium
  • Potassium