Antiarrhythmic and proarrhythmic properties of σ-receptor ligands

Yu B. Lishmanov, L. N. Maslov, A. V. Krylatov, D. S. Ugdyzhekova, P. Giligan, S. T. Tam

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It has been found that the σ1- and σ3-receptor antagonists, DuP 734 intraperitoneally and XJ 448 intravenously, had antiarrhythmic effects against epinephrine-induced arrhythmias in rats. The ED50 for antiarrhythmic effect of DuP 734 was 0.157 mg/kg after intraperitoneal administration. Other σ-receptor antagonists (rimcazole, BMY 14802, haloperidol) did not affect the incidence of epinephrine-induced arrhythmias. σ1-Receptor agonists (DTG, N-allyl-normetazocine, (+)-3-PPP, (-)-3-PPP) had proarrhythmic effect after systemic administration. The σ-agonist N-allyl-normetazocine and σ-antagonist XJ 488 had no effect on the incidence of epinephrine-induced arrhythmias after intracerebroventricular administration. Therefore, it appears that the central nervous system does not play a significant role in the antiarrhythmic or proarrhythmic effects of σ-ligands. We hypothesize that these effects of σ-ligands might be dependent on their action on cardiac σ-receptors.

Original languageEnglish
Pages (from-to)43
Number of pages1
JournalEksperimental'naya i Klinicheskaya Farmakologiya
Issue number2
Publication statusPublished - 2000

ASJC Scopus subject areas

  • Pharmacology, Toxicology and Pharmaceutics(all)

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