A novel type of internal barium block of a maxi-K+ channel from human vas deferens epithelial cells

Biophys J. 1998 Jan;74(1):199-209. doi: 10.1016/S0006-3495(98)77780-X.

Abstract

We have recently shown that a maxi-K+ channel from vas deferens epithelial cells contains two Ba2+-binding sites accessible from the external side: a "flickering" site located deep in the channel pore and a "slow" site located close to the extracellular mouth of the channel. Using the patch-clamp technique, we have now studied the effect of internal Ba2+ on this channel. Cytoplasmic Ba2+ produced a voltage- and concentration-dependent "slow" type of block with a dissociation constant of approximately 100 microM. However, based on its voltage dependence and sensitivity to K+ concentration, this block was clearly different from the external "slow" Ba2+ block previously described. Kinetic analysis also revealed a novel "fast flickering" block restricted to channel bursts, with an unblocking rate of approximately 310 s(-1), some 10-fold faster than the external "flickering" block. Taken together, these results show that this channel contains multiple Ba2+-binding sites within the conduction pore. We have incorporated this information into a new model of Ba2+ block, a novel feature of which is that internal "slow" block results from the binding of at least two Ba2+ ions. Our results suggest that current models for Ba2+ block of maxi-K+ channels need to be revised.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Barium / pharmacology*
  • Binding Sites
  • Cells, Cultured
  • Epithelial Cells / physiology*
  • Humans
  • Ion Channel Gating
  • Kinetics
  • Large-Conductance Calcium-Activated Potassium Channels
  • Male
  • Membrane Potentials / drug effects
  • Models, Biological
  • Potassium / pharmacology
  • Potassium Channel Blockers
  • Potassium Channels / chemistry
  • Potassium Channels / physiology*
  • Potassium Channels, Calcium-Activated*
  • Time Factors
  • Vas Deferens / physiology*

Substances

  • Large-Conductance Calcium-Activated Potassium Channels
  • Potassium Channel Blockers
  • Potassium Channels
  • Potassium Channels, Calcium-Activated
  • Barium
  • Potassium