Abstract
We studied the ability of the agonist of κ1-opioid receptors U-50,488 in doses of 0.1 and 1 mg/kg to simulate ischemic pre- and postconditioning of the heart and κ-opioid receptors ICI 199,441 in a dose of 0.1 mg/kg to simulate the antiarrhythmic effect of heart preconditioning. The duration of ischemia was 10 or 45 min and the duration of reperfusion was 10 min or 2 h. Administration of 1 mg/kg U-50,488 both before ischemia and 5 min before reperfusion produced a pronounced antiarrhythmic effect. U-50,488 injected 5 min before reperfusion 2-fold reduced the ratio of infarction to risk area. Administration of ICI 199,441 in a dose of 0.1 mg/kg 15 min before ischemia produced a potent antiarrhythmic effect. Antiarrhythmic effect of κ-opioid receptor agonists depended on activation of κ-opioid receptors.
Keywords:
heart; postconditioning; reperfusion; κ-opioid receptors.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer / pharmacology*
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3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer / therapeutic use
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Animals
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Anti-Arrhythmia Agents / pharmacology
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Anti-Arrhythmia Agents / therapeutic use
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Cardiotonic Agents / pharmacology*
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Cardiotonic Agents / therapeutic use
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Ischemic Preconditioning, Myocardial / methods*
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Myocardial Ischemia / drug therapy
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Myocardial Ischemia / pathology
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Myocardial Reperfusion Injury / prevention & control*
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Pyrrolidines / pharmacology*
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Pyrrolidines / therapeutic use
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Rats
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Rats, Wistar
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Receptors, Opioid, kappa / agonists*
Substances
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Anti-Arrhythmia Agents
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Cardiotonic Agents
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Pyrrolidines
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Receptors, Opioid, kappa
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kappa(1) opioid receptor
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ICI 199441
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3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer