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 |
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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 journal › Article
}
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.
UR - http://www.scopus.com/inward/record.url?scp=0043197332&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0043197332&partnerID=8YFLogxK
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 -