Use dependent depression of fast sodium current in heart muscle by the new antiarrhythmic substance Bonnecor (AWD 19-166, GS 015)

Pharmazie. 1985 Dec;40(12):852-4.

Abstract

A new antiarrhythmic compound (Bonnecor AWD 19-166, GS 015) was studied in its effects on the fast sodium channel in two types of cardiac preparations (rabbit ventricular myocardium, frog atrial trabecules). AWD 19-166 depressed the maximum upstroke velocity of the action potentials in ventricular myocardium (50% inhibition at 5 X 10(-6) mol/l) and decreased the fast inward current in frog atrial myocardium. High frequent trains of pacing pulses produced a pacing dependent extra block of both the maximal upstroke velocity and the fast inward current. It is concluded that AWD 19-166 blocks the fast sodium channel in a use dependent manner.

MeSH terms

  • Action Potentials / drug effects
  • Animals
  • Anti-Arrhythmia Agents / pharmacology*
  • Dibenzazepines / pharmacology*
  • Heart / drug effects*
  • In Vitro Techniques
  • Ion Channels / drug effects*
  • Kinetics
  • Myocardium / metabolism
  • Rabbits
  • Ranidae

Substances

  • Anti-Arrhythmia Agents
  • Dibenzazepines
  • Ion Channels
  • tiracizine