[The anti-arrhythmic effect of the selective sigma-receptor antagonist DuP 734 [1-(cyclopropylmethyl)-4-(2'-(4''-fluorophenyl)-2'-oxoethyl)piper idine HBr]]

Eksp Klin Farmakol. 1997 Mar-Apr;60(2):24-6.
[Article in Russian]

Abstract

It was demonstrated on models of epinephrine-, CaCl2-, and aconitine-induced arrhythmias that the sigma-receptor antagonist DuP734 possesses high antiarrhythmic activity in a dose of 1 mg/kg. The sigma-receptor agonist-(+)SKF10,047 promoted the development of ventricular fibrillation. Atropine had no effect on the antiarrhythmic properties of DuP734. "Chemical sympathectomy" of the myocardium with the ganglion-blocking agent hexamethonium also did not affect the proarrhythmic properties of (+)SKF10,047. It is supposed that selective sigma-receptor blocking agents may be highly effective antiarrhythmic drugs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aconitine
  • Animals
  • Anti-Arrhythmia Agents / therapeutic use*
  • Arrhythmias, Cardiac / chemically induced
  • Arrhythmias, Cardiac / drug therapy
  • Calcium Chloride
  • Disease Models, Animal
  • Drug Evaluation, Preclinical
  • Epinephrine
  • Ligands
  • Male
  • Phenazocine / analogs & derivatives
  • Phenazocine / therapeutic use
  • Piperidines / therapeutic use*
  • Rats
  • Rats, Wistar
  • Receptors, sigma / agonists
  • Receptors, sigma / antagonists & inhibitors
  • Receptors, sigma / drug effects*
  • Serotonin Antagonists / therapeutic use*

Substances

  • Anti-Arrhythmia Agents
  • Ligands
  • Piperidines
  • Receptors, sigma
  • Serotonin Antagonists
  • SK&F 10047
  • DuP 734
  • Phenazocine
  • Calcium Chloride
  • Aconitine
  • Epinephrine