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首页> 美国卫生研究院文献>CNS Drug Reviews >Neuroprotective Effects of Edaravone: a Novel Free Radical Scavenger in Cerebrovascular Injury
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Neuroprotective Effects of Edaravone: a Novel Free Radical Scavenger in Cerebrovascular Injury

机译：依达拉奉的神经保护作用：脑血管损伤中的新型自由基清除剂。

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Recanalization and neuroprotection have been mainly targeted for the specific treatment of acute ischemic stroke. Free radicals play a crucial role in brain ischemic injury by exacerbating membrane damage through peroxidation of unsaturated fatty acids of cell membrane, leading to neuronal death and brain edema. Free radicals have been implicated in stroke pathophysiology as pivotal contributors to cell injury. Edaravone (3‐methyl‐1‐phenyl‐2‐pyrazolin‐5‐one) is a novel potent free radical scavenger that has been clinically used to reduce the neuronal damage following ischemic stroke. Edaravone exerts neuroprotective effects by inhibiting endothelial injury and by ameliorating neuronal damage in brain ischemia. Edaravone provides the desirable features of NOS: it increases eNOS (beneficial NOS for rescuing ischemic stroke) and decreases nNOS and iNOS (detrimental NOS). Post‐ reperfusion brain edema and hemorrhagic events induced by thrombolytic therapy may be reduced by edaravone pretreatment. Increased productions of superoxide and NO in the brain after reperfusion and a concomitant surge in oxygen free radicals with increased NO during recirculation lead to formation of peroxynitrite, a superpotent radical. Edaravone, which inhibits oxidation and enhances NO production derived from increased eNOS expression, may improve and conserve cerebral blood flow without peroxynitrite generation during reperfusion. Clinical experience with edaravone suggests that this drug has a wide therapeutic time window. The combination therapy (a thrombolytic plus edaravone) is likely to target brain edema, reduce stroke death and improve the recovery from neurological deficits in stoke patients.
机译：再通和神经保护主要针对急性缺血性中风的特异性治疗。自由基通过使细胞膜的不饱和脂肪酸过氧化加剧膜损伤，从而导致神经元死亡和脑水肿，从而在脑缺血损伤中发挥关键作用。自由基与中风病理生理学有关，是细胞损伤的关键因素。依达拉奉（3-甲基-1-苯基-2-吡唑啉-5-酮）是一种新型的有效自由基清除剂，已在临床上用于减轻缺血性中风后的神经元损害。依达拉奉通过抑制内皮损伤和减轻脑缺血中的神经元损伤而发挥神经保护作用。依达拉奉具有NOS的理想功能：它增加eNOS（用于拯救缺血性卒中的有益NOS），并降低nNOS和iNOS（有害NOS）。依达拉奉预处理可减少再灌注后脑水肿和溶栓治疗引起的出血事件。再灌注后大脑中超氧化物和一氧化氮的产生增加，并伴随着氧自由基的激增，而在再循环过程中一氧化氮的增加导致了过氧亚硝酸盐（一种超强自由基）的形成。依达拉奉可抑制氧化并增强由eNOS表达增加引起的NO产生，可改善并保存脑血流，而在再灌注期间不会产生过亚硝酸盐。依达拉奉的临床经验表明，该药物具有广阔的治疗时间范围。组合疗法（溶栓加依达拉奉）可能针对脑水肿，减少中风死亡并改善中风患者神经功能缺损的恢复。

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