title: Prospects of Using of κ-Opioid Receptor Agonists U-50,488 and ICI 199,441 for Improving Heart Resistance to Ischemia/Reperfusion.
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.
authors.affiliation: Research Institute of Cardiology, Tomsk, Russia.|National Research Tomsk Polytechnic University, Tomsk, Russia.
authors.forename: S Yu
authors.initials: SY
authors.lastname: Tsibulnikov
authors.affiliation: Research Institute of Cardiology, Tomsk, Russia. maslov@cardio-tomsk.ru.|National Research Tomsk Polytechnic University, Tomsk, Russia. maslov@cardio-tomsk.ru.
authors.forename: L N
authors.initials: LN
authors.lastname: Maslov
authors.affiliation: Research Institute of Cardiology, Tomsk, Russia.
authors.forename: A V
authors.initials: AV
authors.lastname: Mukhomedzyanov
authors.affiliation: Research Institute of Cardiology, Tomsk, Russia.|National Research Tomsk Polytechnic University, Tomsk, Russia.
authors.forename: A V
authors.initials: AV
authors.lastname: Krylatov
authors.affiliation: National Research Tomsk Polytechnic University, Tomsk, Russia.
authors.forename: M R
authors.initials: MR
authors.lastname: Tsibulnikova
authors.affiliation: Research Institute of Cardiology, Tomsk, Russia.|National Research Tomsk Polytechnic University, Tomsk, Russia.
authors.forename: Yu B
authors.initials: YB
authors.lastname: Lishmanov
mesh_terms: D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000494:pharmacology / Q000627:therapeutic use; D002316:Cardiotonic Agents / Q000494:pharmacology* / Q000627:therapeutic use; D019157:Ischemic Preconditioning, Myocardial / Q000379:methods*; D017202:Myocardial Ischemia / Q000188:drug therapy / Q000473:pathology; D015428:Myocardial Reperfusion Injury / Q000517:prevention & control*; D011759:Pyrrolidines / Q000494:pharmacology* / Q000627:therapeutic use; D051381:Rats; D017208:Rats, Wistar; D017473:Receptors, Opioid, kappa / Q000819:agonists*
chemical_list: D000889:Anti-Arrhythmia Agents; D002316:Cardiotonic Agents; D011759:Pyrrolidines; D017473:Receptors, Opioid, kappa; C116587:kappa(1) opioid receptor; C058468:ICI 199441; D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer
keywords: heart; postconditioning; reperfusion; κ-opioid receptors