About specificity of the antiarrhythmic effect of κ1-opioid receptor agonists

D. S. Ugdyzhekova, L. N. Maslov, A. V. Krylatov, Yu B. Lishmanov, S. W. Tam

Research output: Contribution to journalArticle

Abstract

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.

Original languageEnglish
Pages (from-to)20
Number of pages1
JournalEksperimental'naya i Klinicheskaya Farmakologiya
Volume64
Issue number4
Publication statusPublished - 2001

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Opioid Receptors
Reperfusion
Cardiac Arrhythmias
Myocardial Reperfusion
Coronary Occlusion
Intravenous Administration
Epinephrine
Rats
Coronary Vessels
Myocardium
Ischemia
Incidence

ASJC Scopus subject areas

  • Pharmacology, Toxicology and Pharmaceutics(all)

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About specificity of the antiarrhythmic effect of κ1-opioid receptor agonists. / Ugdyzhekova, D. S.; Maslov, L. N.; Krylatov, A. V.; Lishmanov, Yu B.; Tam, S. W.

In: Eksperimental'naya i Klinicheskaya Farmakologiya, Vol. 64, No. 4, 2001, p. 20.

Research output: Contribution to journalArticle

Ugdyzhekova, D. S. ; Maslov, L. N. ; Krylatov, A. V. ; Lishmanov, Yu B. ; Tam, S. W. / About specificity of the antiarrhythmic effect of κ1-opioid receptor agonists. In: Eksperimental'naya i Klinicheskaya Farmakologiya. 2001 ; Vol. 64, No. 4. pp. 20.
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AU - Ugdyzhekova, D. S.

AU - Maslov, L. N.

AU - Krylatov, A. V.

AU - Lishmanov, Yu B.

AU - Tam, S. W.

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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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