TY - JOUR
T1 - Antiarrhythmic and proarrhythmic properties of σ-receptor ligands
AU - Lishmanov, Yu B.
AU - Maslov, L. N.
AU - Krylatov, A. V.
AU - Ugdyzhekova, D. S.
AU - Giligan, P.
AU - Tam, S. T.
PY - 2000
Y1 - 2000
N2 - 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.
AB - 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.
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M3 - Article
AN - SCOPUS:0043187836
VL - 63
SP - 43
JO - Eksperimental'naya i Klinicheskaya Farmakologiya
JF - Eksperimental'naya i Klinicheskaya Farmakologiya
SN - 0869-2092
IS - 2
ER -