Selective modulation of the ATP-sensitive K+ channel by nicorandil in guinea-pig cardiac cell membrane

Naunyn Schmiedebergs Arch Pharmacol. 1990 Nov;342(5):592-7. doi: 10.1007/BF00169050.

Abstract

Effects of a vasodilator, nicorandil (2-nicotinamidoethyl nitrate) on four kinds for cardiac K+ channels were investigated in guinea pig ventricular and atrial cells using inside-out patch recording combined with "oil-gate" concentration jump method. Nicorandil of 300 mumols/l failed to affect the inward-rectifier K+ channel and the Na(+)-activated K+ channel. The open probability of the muscarinic K+ channel, when activated by the application of GTP, was not changed by the drug. Nicorandil selectively increased the open probability of the ATP-sensitive K+ channel that was partly suppressed by intracellular ATP. The median effective concentration (EC50) of nicorandil was 74 mumols/l and Hill coefficient was 1.32 in the concentration-open probability relationship. The closing rate of the K+ channel by ATP was markedly delayed by the drug, whereas the open rate on removal of ATP was scarcely affected. Nicorandil had only little effect on this channel after run-down. It was concluded that nicorandil selectively activates the ATP-sensitive K+ channel mainly by modulating the ATP-dependent gate.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Triphosphate / physiology*
  • Animals
  • Cell Membrane / drug effects
  • Guinea Pigs
  • Heart / drug effects*
  • In Vitro Techniques
  • Kinetics
  • Myocardium / cytology
  • Niacinamide / analogs & derivatives*
  • Niacinamide / pharmacology
  • Nicorandil
  • Potassium Channels / drug effects*
  • Potassium Channels / physiology
  • Vasodilator Agents / pharmacology*

Substances

  • Potassium Channels
  • Vasodilator Agents
  • Niacinamide
  • Nicorandil
  • Adenosine Triphosphate