TY - JOUR
T1 - About specificity of the antiarrhythmic effect of κ1-opioid receptor agonists
AU - Ugdyzhekova, D. S.
AU - Maslov, L. N.
AU - Krylatov, A. V.
AU - Lishmanov, Yu B.
AU - Tam, S. W.
PY - 2001
Y1 - 2001
N2 - It is demonstrated that intravenous administration of the κ1-opioid receptor (OR) agonists (-)-trans-(1S,S)-U-50,488 and (+)-trans-(1R,2R)-U-50,488 increases heart tolerance to the arrhythmogenic effect of epinephrine in rats. This antiarrhythmic effect was completely abolished by preliminary κ-OR blocking with norbinaltorphimine. Preliminary administration of of a high-affinity κ1-OR agonist (-)-trans-(1S,S)-U-50,488 significantly reduced the incidence of ventricular arrhythmias upon coronary artery occlusion and reperfusion in vivo. The low-affinity (+)-trans-(1R,2R)-U-50,488 does not show antiarrhythmic activity under ischemia and reperfusion of myocardium. It is concluded that the antiarrhythmic action of κ1-OR agonists in the adrenal, ischemic, and reperfusion arrhythmia models has a receptor-specific character.
AB - It is demonstrated that intravenous administration of the κ1-opioid receptor (OR) agonists (-)-trans-(1S,S)-U-50,488 and (+)-trans-(1R,2R)-U-50,488 increases heart tolerance to the arrhythmogenic effect of epinephrine in rats. This antiarrhythmic effect was completely abolished by preliminary κ-OR blocking with norbinaltorphimine. Preliminary administration of of a high-affinity κ1-OR agonist (-)-trans-(1S,S)-U-50,488 significantly reduced the incidence of ventricular arrhythmias upon coronary artery occlusion and reperfusion in vivo. The low-affinity (+)-trans-(1R,2R)-U-50,488 does not show antiarrhythmic activity under ischemia and reperfusion of myocardium. It is concluded that the antiarrhythmic action of κ1-OR agonists in the adrenal, ischemic, and reperfusion arrhythmia models has a receptor-specific character.
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M3 - Article
AN - SCOPUS:0043197332
VL - 64
SP - 20
JO - Eksperimental'naya i Klinicheskaya Farmakologiya
JF - Eksperimental'naya i Klinicheskaya Farmakologiya
SN - 0869-2092
IS - 4
ER -