{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,8,18]],"date-time":"2026-08-18T04:08:33Z","timestamp":1787026113560,"version":"build-2736575974"},"reference-count":26,"publisher":"Institute of Physiology of the Czech Academy of Sciences","content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Physiol Res"],"abstract":"<jats:p>The role of opioid \u03ba1 and \u03ba2 receptors in reperfusion cardiac injury was studied. Male Wistar rats were subjected to a 45-min coronary artery occlusion followed by a 120-min reperfusion. Opioid \u03ba receptor agonists were administered intravenously 5 min before the onset of reperfusion, while opioid receptor antagonists were given 10 min before reperfusion. The average value of the infarct size\/area at risk (IS\/AAR) ratio was 43 \u2013 48 % in untreated rats. Administration of the opioid \u03ba1 receptor agonist (-)-U-50,488 (1 mg\/kg) limited the IS\/AAR ratio by 42 %. Administration of the opioid \u03ba receptor agonist ICI 199,441 (0.1 mg\/kg) limited the IS\/AAR ratio by 41 %. The non-selective opioid \u03ba receptor agonist (+)-U-50,488 (1 mg\/kg) with low affinity for opioid \u03ba receptor, the peripherally acting opioid \u03ba receptor agonist ICI 204,448 (4 mg\/kg) and the selective opioid \u03ba2 receptor agonist GR89696 (0.1 mg\/kg) had no effect on the IS\/AAR ratio. Pretreatment with naltrexone, the peripherally acting opioid receptor antagonist naloxone methiodide, or the selective opioid \u03ba receptor antagonist nor-binaltorphimine completely abolished the infarct-reducing effect of (-)-U-50,488 and ICI 199,441. Pretreatment with the selective opioid \u03b4 receptor antagonist TIPP[\u03c8] and the selective opioid \u00b5 receptor antagonist CTAP did not alter the infarct reducing effect of (-)-U-50,488 and ICI 199,441. Our study is the first to demonstrate the following: (a) the activation of opioid \u03ba2 receptor has no effect on cardiac tolerance to reperfusion; (b) peripheral opioid \u03ba1 receptor stimulation prevents reperfusion cardiac injury; (c) ICI 199,441 administration resulted in an infarct-reducing effect at reperfusion; (e) bradycardia induced by opioid \u03ba receptor antagonists is not dependent on the occupancy of opioid \u03ba receptor.<\/jats:p>","DOI":"10.33549\/physiolres.934646","type":"journal-article","created":{"date-parts":[[2021,9,2]],"date-time":"2021-09-02T07:25:20Z","timestamp":1630567520000},"page":"523-531","source":"Crossref","is-referenced-by-count":8,"title":["Activation of peripheral opioid \u03ba1 receptor prevents cardiac reperfusion injury"],"prefix":"10.33549","author":[{"given":"Sergey V.","family":"Popov","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Alexander V.","family":"Mukhomedzyanov","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sergey Y.","family":"Tsibulnikov","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Igor","family":"Khaliulin","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Peter R.","family":"Oeltgen","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"N.","family":"Rajendra Prasad","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Leonid N.","family":"Maslov","sequence":"additional","affiliation":[{"name":"Laboratory of Experimental Cardiology, Cardiology Research Institute, Tomsk National Research Medical Center, the Russian Academy of Sciences, Tomsk, Russia. maslov@cardio-tomsk.ru"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"19169","published-online":{"date-parts":[[2021,8,31]]},"reference":[{"key":"ref0","doi-asserted-by":"publisher","unstructured":"BARLOW JJ, BLACKBURN TP, COSTELLO GF, JAMES R, LE COUNT DJ, MAIN BG, PEARCE RJ, RUSSELL K, SHAW JS: Structure\/activity studies related to 2-(3,4-dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted-ethyl]acetamides: a novel series of potent and selective kappa-opioid agonists. 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