How is edaravone effective against acute ischemic stroke and amyotrophic lateral sclerosis?

How is edaravone effective against acute ischemic stroke and amyotrophic lateral sclerosis?
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Edaravone如何对急性缺血性中风和肌萎缩性侧索硬化有效?

DOI:
10.3164/jcbn.17-62
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发表时间:
2018-01
影响因子:
2.4
通讯作者:
Yamamoto Y
Yamamoto Y
中科院分区:
医学4区
文献类型:
--
作者:
Watanabe K;Tanaka M;Yuki S;Hirai M;Yamamoto Y

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依达拉奉是一种针对多种类型的活性氧中的过氧化自由基的低分子抗氧化剂。由于它的两亲性,它通过给自由基提供一个电子来清除脂类和水溶性的过氧基。因此,它通过清除链引发的水溶性过氧化自由基和链携带的脂质过氧化自由基来抑制脂质的氧化。2001年,它在日本被批准为治疗急性期脑梗塞的药物,然后在2015年,它被批准用于肌萎缩侧索硬化症(ALS)。2017年,美国食品和药物管理局也批准依达拉奉用于治疗ALS患者。其作用机制可能与清除过亚硝酸根有关。本文就依达拉奉清除自由基的特性与临床研究中的其他抗氧化剂进行了比较,并对其在急性脑梗塞和ALS患者中的药理作用和临床疗效进行了综述。
Edaravone is a low-molecular-weight antioxidant drug targeting peroxyl radicals among many types of reactive oxygen species. Because of its amphiphilicity, it scavenges both lipid- and water-soluble peroxyl radicals by donating an electron to the radical. Thus, it inhibits the oxidation of lipids by scavenging chain-initiating water-soluble peroxyl radicals and chain-carrying lipid peroxyl radicals. In 2001, it was approved in Japan as a drug to treat acute-phase cerebral infarction, and then in 2015 it was approved for amyotrophic lateral sclerosis (ALS). In 2017, the U.S. Food and Drug Administration also approved edaravone for treatment of patients with ALS. Its mechanism of action was inferred to be scavenging of peroxynitrite. In this review, we focus on the radical-scavenging characteristics of edaravone in comparison with some other antioxidants that have been studied in clinical trials, and we summarize its pharmacological action and clinical efficacy in patients with acute cerebral infarction and ALS.
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发表时间: 1978-01-01
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