Cardiology Research Institute, Tomsk National Research Medical Centre, Russian Academy of Sciences, Tomsk, Russia.
Bull Exp Biol Med. 2021 Mar;170(5):594-597. doi: 10.1007/s10517-021-05113-7. Epub 2021 Apr 1.
A 45-min coronary artery occlusion followed by a 120-min reperfusion was performed in rats anesthetized with α-chloralose. The selective κ-opioid receptor (OR) agonist U-50,488 was administered intravenously in doses of 0.1 or 1 mg/kg. The selective κ-OR agonist GR-89696 was injected in a dose of 0.1 mg/kg. The selective κ-OR agonists ICI-199,441 and ICI-204,448 were employed in the doses of 0.1 and 4 mg/kg, respectively. These drugs were injected 5 min prior to reperfusion. U-50,488 exerted the cardioprotective effect in a dose of 1 mg/kg, but it produced no effect on infarct size in a dose of 0.1 mg/kg. ICI-199,441 reduced the reperfusion injury to the heart. The infarct size limiting effects of U-50,488 and ICI-199,441 were prevented by preliminary injection of naltrexone or nor-binaltorphimine. It is concluded that infarct size limiting effects of U-50,488 and ICI-199,441 were mediated via activation of κ-OR.
在α-氯醛糖麻醉的大鼠中进行了 45 分钟的冠状动脉闭塞，然后进行 120 分钟的再灌注。静脉内给予选择性 κ 阿片受体（OR）激动剂 U-50,488，剂量为 0.1 或 1mg/kg。给予选择性 κ-OR 激动剂 GR-89696，剂量为 0.1mg/kg。选择性 κ-OR 激动剂 ICI-199,441 和 ICI-204,448 的剂量分别为 0.1 和 4mg/kg。这些药物在再灌注前 5 分钟注射。U-50,488 在 1mg/kg 的剂量下发挥了心脏保护作用，但在 0.1mg/kg 的剂量下对梗死面积没有影响。ICI-199,441 减轻了再灌注对心脏的损伤。预先注射纳洛酮或诺比那尔托米芬可预防 U-50,488 和 ICI-199,441 的梗死面积限制作用。结论：U-50,488 和 ICI-199,441 的梗死面积限制作用是通过激活 κ-OR 介导的。
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