Preferential inhibition of Ih in rat trigeminal ganglion neurons by an organic blocker

J Membr Biol. 1997 Nov 15;160(2):101-9. doi: 10.1007/s002329900299.

Abstract

The potency and specificity of a novel organic Ih current blocker DK-AH 268 (DK, Boehringer) was studied in cultured rat trigeminal ganglion neurons using whole-cell patch-clamp recording techniques. In neurons current-clamped at the resting potential, the application of 10 microM DK caused a slight hyperpolarization of the membrane potential and a small increase in the threshold for action potential discharge without any major change in the shape of the action potential. In voltage-clamped neurons, DK caused a reduction of a hyperpolarization-activated current. Current subtraction protocols revealed that the time-dependent, hyperpolarization-activated currents blocked by 10 microM DK or external Cs+ (3 mM) had virtually identical activation properties, suggesting that DK and Cs+ caused blockade of the same current, namely Ih. The block of Ih by DK was dose-dependent. At the intermediate and higher concentrations of DK (10 and 100 microM) a decrease in specificity was observed so that time-independent, inwardly rectifying and noninactivating, voltage-gated outward potassium currents were also reduced by DK but to a much lesser extent than the time-dependent, hyperpolarization-activated currents. Blockade of the time-dependent, hyperpolarization-activated currents by DK appeared to be use-dependent since it required hyperpolarization for the effect to take place. Relief of DK block was also aided by membrane hyperpolarization. Since both the time-dependent current blocked by DK and the Cs+-sensitive time-dependent current behaved as Ih, we conclude that 10 microM DK can preferentially reduce Ih without a major effect on other potassium currents. Thus, DK may be a useful agent in the investigation of the function of Ih in neurons.

Publication types

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

MeSH terms

  • Action Potentials / drug effects
  • Animals
  • Benzazepines / pharmacology*
  • Cells, Cultured
  • Cesium / pharmacology
  • Membrane Potentials / drug effects
  • Neurons / drug effects
  • Neurons / physiology
  • Patch-Clamp Techniques
  • Potassium / metabolism
  • Potassium Channel Blockers
  • Potassium Channels / metabolism
  • Rats
  • Sodium / metabolism
  • Trigeminal Ganglion / cytology
  • Trigeminal Ganglion / drug effects*
  • Trigeminal Ganglion / physiology*

Substances

  • Benzazepines
  • Potassium Channel Blockers
  • Potassium Channels
  • DK-AH 268
  • Cesium
  • Sodium
  • Potassium