[Inhibition of transmembrane K(+) currents in mammalian ventricular myocytes by antiarrhythmic agent RP62719]

Sheng Li Xue Bao. 2000 Oct;52(5):427-30.
[Article in Chinese]

Abstract

The effect of RP62719 on the inward rectifier K(+) current (I(K1)),transient outward K(+) current (I(to)) and delayed outward K(+) current (I(K)) in isolated cardiac myocytes was determined using the whole cell patch clamp technique in guinea pig and dog. RP62719 decreased I(K1) with an inhibitory concentration 50 (IC(50) ) of 5.0+/-1.0 micromol/L at -100 mV in guinea pig ventricular cells. In dog ventricular myocytes, RP62719 inhibited Ito by 84+/-4.4% with an IC(50) of 1.2+/-0.51 micromol/L at +40 mV. In guinea pig ventricular cells, RP62719 decreased I(K): I(Kstep) by 50.0+/-8.3%%and I(Ktail) by 56.0+/-4.9% at +40 mV, respectively. RP62719 inhibited I(Kstep) with an IC(50) of 4.2+/-0.8 micromol/L and I(Ktail) with an IC(50) of 3.3+/-0.75 micromol/L. Thus it is suggested that the ionic mechanism of antiarrhymic effect by RP62719 may be due to its inhibition of I(K1),I(to) and I(K).

Publication types

  • English Abstract

MeSH terms

  • Animals
  • Anti-Arrhythmia Agents / pharmacology*
  • Cell Separation
  • Chromans / pharmacology*
  • Dogs
  • Guinea Pigs
  • Heart Ventricles / cytology
  • Inhibitory Concentration 50
  • Myocytes, Cardiac / drug effects*
  • Myocytes, Cardiac / physiology
  • Patch-Clamp Techniques
  • Piperidines / pharmacology*
  • Potassium Channels / drug effects*
  • Potassium Channels, Inwardly Rectifying / drug effects*

Substances

  • Anti-Arrhythmia Agents
  • Chromans
  • Piperidines
  • Potassium Channels
  • Potassium Channels, Inwardly Rectifying
  • terikalant