title: [The anti-arrhythmia and pro-arrhythmia properties of sigma-receptor ligands].
abstract: It has been found that the sigma 1- and sigma 3-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 sigma-receptor antagonists (rimcazole, BMY 14802, haloperidol) did not affect the incidence of epinephrine-induced arrhythmias. sigma 1-Receptor agonists (DTG, N-allyl-normetazocine, (+)-3-PPP, (-)-3-PPP) had proarrhythmic effect after systemic administration. The sigma-agonist N-allyl-normetazocine and sigma-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 sigma ligands. We hypothesize that these effects of sigma ligands might be dependent on their action on cardiac sigma receptors.
authors.affiliation: Department of Experimental Cardiology, Tomsk Scientific Center, Siberian Division, Russian Academy of Medical Sciences, Russia.
authors.forename: Iu B
authors.initials: IuB
authors.lastname: Lishmanov
authors.forename: L N
authors.initials: LN
authors.lastname: Maslov
authors.forename: A V
authors.initials: AV
authors.lastname: Krylatov
authors.forename: D S
authors.initials: DS
authors.lastname: Ugdyzhekova
authors.forename: P
authors.initials: P
authors.lastname: Gilligan
authors.forename: S W
authors.initials: SW
authors.lastname: Tam
mesh_terms: D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000494:pharmacology / Q000627:therapeutic use*; D001145:Arrhythmias, Cardiac / Q000139:chemically induced / Q000188:drug therapy*; D004195:Disease Models, Animal; D004353:Drug Evaluation, Preclinical; D004562:Electrocardiography / Q000187:drug effects; D004837:Epinephrine; D008024:Ligands; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D017480:Receptors, sigma / Q000819:agonists* / Q000037:antagonists & inhibitors* / Q000187:drug effects
chemical_list: D000889:Anti-Arrhythmia Agents; D008024:Ligands; D017480:Receptors, sigma; D004837:Epinephrine