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3-甲基-1-苯基-2-吡唑啉-5-酮(依达拉奉)的构效关系

Structure-activity relationship of 3-methyl-1-phenyl-2-pyrazolin-5-one (edaravone).

作者信息

Watanabe Kazutoshi, Morinaka Yasuhiro, Iseki Katsuhiko, Watanabe Toshiaki, Yuki Satoshi, Nishi Hiroyoshi

机构信息

Research and Development Division, Mitsubishi Pharma Corporation, Yokohama, Japan.

出版信息

Redox Rep. 2003;8(3):151-5. doi: 10.1179/135100003225001520.

DOI:10.1179/135100003225001520
PMID:12935312
Abstract

This paper describes the discovery of a novel free radical scavenger, 3-methyl-1-phenyl-2-pyrazolin-5-one (edaravone, 1), as a potent antioxidant agent against lipid peroxidation. The structure-activity relationship of edaravone indicated that lipophilic substituents were essential to show its lipid peroxidation-inhibitory activity. In vivo studies revealed that edaravone showed brain-protective activity in a transient ischemia model.

摘要

本文描述了一种新型自由基清除剂3-甲基-1-苯基-2-吡唑啉-5-酮(依达拉奉,1)作为一种有效的抗脂质过氧化抗氧化剂的发现。依达拉奉的构效关系表明,亲脂性取代基对于表现出其脂质过氧化抑制活性至关重要。体内研究表明,依达拉奉在短暂性脑缺血模型中显示出脑保护活性。

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Structure-activity relationship of 3-methyl-1-phenyl-2-pyrazolin-5-one (edaravone).3-甲基-1-苯基-2-吡唑啉-5-酮(依达拉奉)的构效关系
Redox Rep. 2003;8(3):151-5. doi: 10.1179/135100003225001520.
2
Radical scavenger edaravone developed for clinical use ameliorates ischemia/reperfusion injury in rat kidney.用于临床的自由基清除剂依达拉奉可改善大鼠肾脏缺血/再灌注损伤。
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Pulse radiolysis study on free radical scavenger edaravone (3-methyl-1-phenyl-2-pyrazolin-5-one). 2: A comparative study on edaravone derivatives.脉冲辐解研究自由基清除剂依达拉奉(3-甲基-1-苯基-2-吡唑啉-5-酮)。2:依达拉奉衍生物的比较研究。
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Edaravone inhibits lipid peroxidation in neonatal hypoxic-ischemic rats: an in vivo microdialysis study.依达拉奉抑制新生缺氧缺血性大鼠的脂质过氧化:一项体内微透析研究。
Neurosci Lett. 2007 Feb 27;414(1):5-9. doi: 10.1016/j.neulet.2006.10.024. Epub 2007 Feb 5.
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Edaravone (3-methyl-1-phenyl-2-pyrazolin-5-one), a radical scavenger, prevents 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-induced neurotoxicity in the substantia nigra but not the striatum.依达拉奉(3-甲基-1-苯基-2-吡唑啉-5-酮)是一种自由基清除剂,可预防1-甲基-4-苯基-1,2,3,6-四氢吡啶诱导的黑质神经毒性,但对纹状体无此作用。
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Edaravone, a newly developed radical scavenger, protects against ischemia-reperfusion injury of the small intestine in rats.依达拉奉是一种新开发的自由基清除剂,可保护大鼠小肠免受缺血再灌注损伤。
Int J Mol Med. 2004 Jan;13(1):105-9.
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Repeated edaravone treatment reduces oxidative cell damage in rat brain induced by middle cerebral artery occlusion.反复给予依达拉奉治疗可减轻大脑中动脉闭塞诱导的大鼠脑氧化细胞损伤。
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[Research and development of the free radical scavenger edaravone as a neuroprotectant].自由基清除剂依达拉奉作为神经保护剂的研发
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Effect of the free radical scavenger, 3-methyl-1-phenyl-2-pyrazolin-5-one (MCI-186), on hypoxia-ischemia-induced brain injury in neonatal rats.
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A theoretical investigation on DPPH radical-scavenging mechanism of edaravone.依达拉奉对DPPH自由基清除机制的理论研究
Bioorg Med Chem Lett. 2003 Nov 3;13(21):3789-92. doi: 10.1016/j.bmcl.2003.07.016.

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