Antiarrhythmic action of the new calcium antagonist [1,2,5-trimethyl-4-phenyl-4-beta-(N-cyanoethyl-N-4'-methoxybenzyl) -ethylamino]piperidine dihydrochloride

Arzneimittelforschung. 1996 Dec;46(12):1110-3.

Abstract

Arrhythmias induced by coronary artery ligation in cats, by CaCl2 and epinephrine in rats, and by ouabain in guinea-pigs were used as experimental models for studying the effects of a new calcium antagonist AR-1 ([1,2,5-trimethyl-4-phenyl-4-beta-(N-cyanoethyl-N-4'-methoxybenzyl) -ethylamino]piperidine, calcium channel blocker and calmodulin antagonist) on ventricular arrhythmias. Coronary ligation caused 90% lethality (ventricular fibrillation) with 12.5 min in untreated control cats, which was prevented by administration of AR-1 (4 mg/kg body weight (b.w.) before or after arrhythmia induction. Pretreatment with AR-1 afforded protection in a dose-related fashion. A dose of 1.5 mg/KG b.w. increased survival to 45%, and all cats dosed with 3 to 5 mg/Kg b.w. survived. CaCl2 (180 mg/Kg b.w., i.v.) induced ventricular fibrillation and 100% lethality. These effects were completely prevented by an anti-arrhythmic dose of AR-1 (3 mg/kg b.w.). Epinephrine-induced ventricular arrhythmias were also prevented by the same dose of AR-1. AR-1 (5 mg/kg b.w.) did not prevent ouabain (0.5 mg/kg b.w.)-induced arrhythmias that caused death within 17 +/- 3.7 min, but displayed protective effects during 67 +/- 7.7 min. The results from these animal studies, in conjunction with previously studies demonstrating coronarodilatory and anti-platelet efficacy of this compound, collectively suggest that AR-1 has a potential to become a useful antianginal and antiarrhythmic therapeutic agent.

MeSH terms

  • Animals
  • Anti-Arrhythmia Agents / pharmacology*
  • Arrhythmias, Cardiac / chemically induced
  • Arrhythmias, Cardiac / drug therapy
  • Arrhythmias, Cardiac / physiopathology
  • Calcium Channel Blockers / pharmacology*
  • Calcium Chloride
  • Cardiovascular Agents
  • Coronary Vessels / physiology
  • Electrocardiography / drug effects
  • Epinephrine
  • Male
  • Ouabain
  • Piperidines / pharmacology*
  • Rats
  • Rats, Wistar
  • Tachycardia, Ventricular / chemically induced
  • Tachycardia, Ventricular / drug therapy
  • Tachycardia, Ventricular / physiopathology
  • Ventricular Fibrillation / physiopathology

Substances

  • AR-1 (antiarrhythmia agent)
  • Anti-Arrhythmia Agents
  • Calcium Channel Blockers
  • Cardiovascular Agents
  • Piperidines
  • Ouabain
  • Calcium Chloride
  • Epinephrine