Delta-opioid receptor antagonists exhibit properties of partial delta-receptor agonists in isolated perfused heart.

Abstract

Perfusion of the isolated intact rat heart with Krebs-Henseleit solution containing agonists ((-)-TAN-67, DPDPE, and dalargin) or antagonists of delta-opioid receptors (naltrindole, TIPP[psi], and ICI 174,864) in a final concentration of 0.1 mg/liter was followed by a decrease in the heart rate, end-diastolic pressure, contraction rate, relaxation rate, and left ventricular developed pressure. Perfusion with a solution containing the delta-opioid receptor agonist DPDPE or delta-antagonists naltrindole, TIPP[psi], and ICI 174,864 before modeling of global ischemia increased the severity of reperfusion-induced contractile dysfunction in the myocardium. Our results suggest that delta-opioid receptor antagonists in vitro exhibit properties of partial delta-receptor agonists.

• Authors: L N Maslov, T V Lasukova, Zh D Bespalova, P Oldgen, K K Rice, H Nagase
• Journal: Bulletin of experimental biology and medicine (Bull Exp Biol Med) Vol. 138 Issue 4 Pg. 376-9 (Oct 2004) ISSN: 0007-4888 [Print] United States
• PMID: 15665949 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Oligopeptides
• Quinolines
• Receptors, Opioid, delta
• TAN 67
• tyrosyl-tetrahydroisoquinolinecarbonyl-psi(methylamino)phenylalanyl-phenylalanine
• Enkephalin, Leucine
• Naltrexone
• Enkephalin, Leucine-2-Alanine
• Enkephalin, D-Penicillamine (2,5)-
• N,N-diallyl-tyrosyl-alpha-aminoisobutyric acid-phenylalanyl-leucine
• naltrindole
• enkephalin-Leu, Ala(2)-Arg(6)-

Topics

• Animals
• Enkephalin, D-Penicillamine (2,5)- (pharmacology)
• Enkephalin, Leucine (analogs & derivatives, pharmacology)
• Enkephalin, Leucine-2-Alanine (analogs & derivatives, pharmacology)
• Heart (drug effects, physiology)
• In Vitro Techniques
• Male
• Myocardial Contraction (drug effects)
• Myocardial Ischemia (physiopathology)
• Naltrexone (analogs & derivatives, pharmacology)
• Oligopeptides (pharmacology)
• Perfusion
• Quinolines (pharmacology)
• Rats
• Rats, Wistar
• Receptors, Opioid, delta (agonists, antagonists & inhibitors, physiology)