We performed a comparative analysis of infarction-limiting activity of analogues of opioid receptor agonist U-50488 under conditions of heart reperfusion in rats. Derivatives of amide N-methyl-2-(pyrrolidin-1-yl)cyclohexyl-1-amine were administered 5 min before reperfusion in a dose of 1 mg/kg, derivative II (opicor) was additionally used in a dose of 2 mg/kg. In a dose of 1 mg/kg, all derivatives of opioid U-50488 were ineffective and produced no infarction-limiting effect. Opicor in a dose of 2 mg/kg reduced the infarction size/area at risk ratio and improved the contractility parameters of the isolated heart. Opioid receptor antagonist naltrexone (5 mg/kg) abolished the infarction-limiting effect of opicor. Hence, the infarction-reducing effect of opicor is associated with activation of opioid receptors. We also demonstrated that the opioid (opicor) can improve cardiac contractility during the reperfusion period.
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Translated from Byulleten’ Eksperimental’noi Biologii i Meditsiny, Vol. 170, No. 12, pp. 686-690, December, 2020
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Mukhomedzyanov, A.V., Zhuk, V.V., Maslov, L.N. et al. Cardioprotective Effect of Opioids, Derivatives of Amide N-Methyl-2-(Pirrolidin-1-yl)Cyclohexyl-1-Amine, under Conditions of Ischemia/Reperfusion of the Heart. Bull Exp Biol Med 170, 710–713 (2021). https://doi.org/10.1007/s10517-021-05138-y
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DOI: https://doi.org/10.1007/s10517-021-05138-y