About specificity of the antiarrhythmic effect of κ<sub>1</sub>-opioid receptor agonists

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 language	English
Pages (from-to)	20
Number of pages	1
Journal	Eksperimental'naya i Klinicheskaya Farmakologiya
Volume	64
Issue number	4
Publication status	Published - 2001

ASJC Scopus subject areas

Pharmacology, Toxicology and Pharmaceutics(all)

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title = "About specificity of the antiarrhythmic effect of κ1-opioid receptor agonists",

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.",

author = "Ugdyzhekova, {D. S.} and Maslov, {L. N.} and Krylatov, {A. V.} and Lishmanov, {Yu B.} and Tam, {S. W.}",

year = "2001",

language = "English",

volume = "64",

pages = "20",

journal = "Eksperimental'naya i Klinicheskaya Farmakologiya",

issn = "0869-2092",

publisher = "Izdatelstvo Meditsina",

number = "4",

}

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 -

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

Abstract

ASJC Scopus subject areas

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