Levosimendan interacts with potassium channel blockers in human saphenous veins

Basic Clin Pharmacol Toxicol. 2004 Jun;94(6):271-3. doi: 10.1111/j.1742-7843.2004.pto940603.x.

Abstract

The involvement of potassium channels in the venodilating capacity of the inodilator levosimendan in human saphenous vein preparations was investigated. Levosimendan caused relaxation with 50% effective concentration (EC50) of 0.32 +/- 0.04 microM in isolated veins contracted by 5-hydroxytryptamine. Fifteen microM glibenclamide, a blocker of the ATP-sensitive potassium channels (K(ATP)), partially inhibited the relaxing effect of the inodilator. In the presence of iberiotoxin, the selective blocker of large conductance calcium-activated potassium channels (BK(Ca)), levosimendan induced contraction with EC50 of 0.21 +/- 0.06 microM. We presume that levosimendan dilates human saphenous veins by interacting with hyperpolarizing potassium channels (K(ATP) and BK(Ca)).

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Drug Interactions
  • Glyburide / pharmacology
  • Humans
  • Hydrazones / pharmacology*
  • In Vitro Techniques
  • Peptides / pharmacology
  • Potassium Channel Blockers / pharmacology*
  • Potassium Channels / drug effects*
  • Potassium Channels / physiology
  • Potassium Channels, Calcium-Activated / drug effects
  • Potassium Channels, Calcium-Activated / physiology
  • Pyridazines / pharmacology*
  • Saphenous Vein / drug effects*
  • Saphenous Vein / physiology
  • Serotonin
  • Simendan
  • Vasodilation / drug effects*
  • Vasodilation / physiology
  • Vasodilator Agents / pharmacology*

Substances

  • Hydrazones
  • Peptides
  • Potassium Channel Blockers
  • Potassium Channels
  • Potassium Channels, Calcium-Activated
  • Pyridazines
  • Vasodilator Agents
  • Serotonin
  • Simendan
  • iberiotoxin
  • Glyburide