The sulphonylurea glibenclamide inhibits voltage dependent potassium currents in human atrial and ventricular myocytes

Br J Pharmacol. 1999 Nov;128(6):1175-80. doi: 10.1038/sj.bjp.0702904.

Abstract

1 It was the aim of our study to investigate the effects of the sulphonylurea glibenclamide on voltage dependent potassium currents in human atrial myocytes. 2 The drug blocked a fraction of the quasi steady state current (ramp response) which was activated positive to -20 mV, was sensitive to 4-aminopyridine (500 microM) and was different from the ATP dependent potassium current IK(ATP). 3 Glibenclamide dose dependently inhibited both, the peak as well as the late current elicited by step depolarization positive to -20 mV. The IC50 for reduction in charge area of total outward current was 76 microM. 4 The double-exponential inactivation time-course of the total outward current was accelerated in the presence of glibenclamide with a tau(fast) of 12.7+/-1.5 ms and a tau(slow) of 213+/-25 ms in control and 5.8+/-1.9 ms (P<0.001) and 101+/-20 ms (P<0.05) under glibenclamide (100 microM). 5 Our data suggest, that both repolarizing currents in human atrial myocytes, the transient outward current (Ito1) and the ultrarapid delayed rectifier current (IKur) were inhibited by glibenclamide. 6 In human ventricular myocytes glibenclamide inhibited Ito1 without affecting the late current. 7 Our data suggest that glibenclamide inhibits human voltage dependent cardiac potassium currents at concentrations above 10 microM.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Triphosphate / physiology
  • Atrial Function
  • Dose-Response Relationship, Drug
  • Electric Stimulation
  • Glyburide / pharmacology*
  • Heart Atria / cytology
  • Heart Atria / drug effects*
  • Heart Ventricles / cytology
  • Heart Ventricles / drug effects*
  • Humans
  • Membrane Potentials / drug effects*
  • Potassium Channels / drug effects*
  • Time Factors
  • Ventricular Function

Substances

  • Potassium Channels
  • Adenosine Triphosphate
  • Glyburide