title: Cardioprotective effect of kappa1-opioid receptor activation and role of cAMP in its realization.
abstract: The cardioprotective and antiarrhythmic effects of a selective kappa1-opioid receptor agonist U-50,488 were studied during experimental 45-min total ischemia and 30-min reperfusion of isolated rat heart. The opioid had no effect on the incidence and type of reperfusion arrhythmias. U-50,488 in a concentration of 0.1 microM inhibited reperfusion-induced release of creatine phosphokinase and decreased cAMP concentration in the myocardium by 2 times. These parameters remained unchanged after treatment with U-50,488 in a concentration of 1 microM. The cardioprotective effect of U-50,488 was probably associated with a decrease in cAMP concentration in heart cells. U-50,488 in a concentration of 1 microM produced no cardioprotective effect, which can be explained by its interaction with an unknown non-opioid receptor in cardiomyocytes.
authors.affiliation: Institute of Cardiology, Tomsk Research Center, Siberian Division of the Russian Academy of Medical Sciences.
authors.forename: T V
authors.initials: TV
authors.lastname: Lasukova
authors.forename: L N
authors.initials: LN
authors.lastname: Maslov
authors.forename: A A
authors.initials: AA
authors.lastname: Platonov
authors.forename: N V
authors.initials: NV
authors.lastname: Guzarova
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*; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000494:pharmacology*; D001145:Arrhythmias, Cardiac / Q000378:metabolism / Q000517:prevention & control*; D003402:Creatine Kinase / Q000378:metabolism; D000242:Cyclic AMP / Q000378:metabolism / Q000502:physiology*; D008297:Male; D015428:Myocardial Reperfusion Injury / Q000378:metabolism / Q000517:prevention & control*; D009206:Myocardium / Q000378:metabolism; D032383:Myocytes, Cardiac / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D017473:Receptors, Opioid, kappa / Q000819:agonists* / Q000502:physiology
chemical_list: D000889:Anti-Arrhythmia Agents; D017473:Receptors, Opioid, kappa; C116587:kappa(1) opioid receptor; D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer; D000242:Cyclic AMP; D003402:Creatine Kinase