KCB-328: a novel class III antiarrhythmic agent with little reverse frequency dependence in isolated guinea pig myocardium

J Cardiovasc Pharmacol. 1998 Apr;31(4):609-17. doi: 10.1097/00005344-199804000-00021.

Abstract

The effects of 1-(2-amino-4-methanesulfonamidophenoxy)-2-[N-(3,4-dimethoxypheneth yl)-N-methylamino] ethane hydrochloride (KCB-328), in comparison with those of dofetilide, were studied on the action potentials (APs) of isolated guinea pig papillary muscles. KCB-328 (0.003-3 microM) concentration-dependently prolonged the AP duration at 90% repolarization (APD90) at 1- and 3-Hz pacing, and the concentration-response relations at 1 and 3 Hz resemble each other. Dofetilide (0.001-1 microM) also produced the concentration-dependent prolongation of APD90 but more pronouncedly at 1 than at 3 Hz, demonstrating the reverse frequency-dependent effect. KCB-328 at 0.03, 0.1, 0.3, and 1 microM increased APD90 by 11 +/- 1, 19 +/- 1, 25 +/- 1, and 29 +/- 1% at 3 Hz and by 9 +/- 1, 19 +/- 2, 27 +/- 2, and 33 +/- 2% at 1 Hz, respectively. Prolongation of the effective refractory period (ERP) by each drug is parallel to those of APD90 at each pacing frequency. KCB-328 modified neither the maximal velocity of depolarization, amplitude of AP, and resting membrane potential in the fast APs, nor any parameters of the slow APs. In a separate experiment, the effects of KCB-328 on the ERP of contractile response (ERPc) of excised guinea-pig papillary muscles also were studied at 1 and 3 Hz. KCB-328 (0.01-10 microM) lengthened the ERPc in a concentration-dependent and frequency-independent manner as in the electrophysiologic results. This frequency-independent ERPc prolongation by KCB-328 was not influenced by increased extracellular K+ concentration from 4 to 10 mM. These results suggest that KCB-328 might be a selective class III agent with effects that are relatively frequency independent.

Publication types

  • Comparative Study

MeSH terms

  • Action Potentials / drug effects
  • Animals
  • Anti-Arrhythmia Agents / pharmacology*
  • Cardiac Pacing, Artificial
  • Dose-Response Relationship, Drug
  • Guinea Pigs
  • Heart / drug effects*
  • In Vitro Techniques
  • Male
  • Myocardial Contraction / drug effects*
  • Neuromuscular Depolarizing Agents / pharmacology
  • Papillary Muscles / drug effects*
  • Phenethylamines / pharmacology*
  • Potassium Channel Blockers*
  • Sulfonamides / pharmacology*

Substances

  • 1-(2-amino-4-methanesulfonamidophenoxy)-2-(N-(3,4-dimethoxyphenethyl)-N-methylamino)ethane
  • Anti-Arrhythmia Agents
  • Neuromuscular Depolarizing Agents
  • Phenethylamines
  • Potassium Channel Blockers
  • Sulfonamides
  • dofetilide