亲爱的研友该休息了!由于当前在线用户较少,发布求助请尽量完整的填写文献信息,科研通机器人24小时在线,伴您度过漫漫科研夜!身体可是革命的本钱,早点休息,好梦!

Research and Development of the Free Radical Scavenger Edaravone as a Neuroprotectant

依达拉奉 自由基清除剂 脂质过氧化 化学 药理学 羟基自由基 氧化应激 激进的 神经保护 缺血 活性氧 生物化学 医学 内科学
作者
Toshiaki Watanabe,Masahiko Tanaka,Kazutoshi Watanabe,Yasuo Takamatsu,Akihiro Tobe
出处
期刊:Journal of the Pharmaceutical Society of Japan 卷期号:124 (3): 99-111 被引量:101
标识
DOI:10.1248/yakushi.124.99
摘要

Increasing data suggest that oxygen free radical species play detrimental roles in ischemic diseases. A free radical scavenger capable of inhibiting oxidative injury is expected to become a new drug for the treatment of ischemic diseases such as cerebral ischemia. Edaravon (3-methyl-1-phenyl-2-pyrazolin-5-one), which has been developed as an neuroprotective agent for more than 15 years since its discovery, is approved for the treatment of acute cerebral infarction. In this paper, the pharmacologic characteristics and clinical effects of edaravone are reviewed. In early stage of investigation, edaravone was found to have promising activities as an antioxidative radical scavenger, quenching hydroxyl radical (.OH) and inhibiting both .OH-dependent and .OH-independent lipid peroxidation. Edaravone showed inhibitory effects on both water-soluble and lipid-soluble peroxyl radical-induced peroxidation systems, which are different from the inhibitory effects of vitamins C and E in each system, respectively. Oxidative injury to cultured endothelial cells caused by arachidonate (AA) peroxides is prevented in the existence of edaravone. To clarify the characteristics of this free radical scavenger, further investigation was carried out. Edaravone ameliorated exacerbation of cortical edema induced by a focal ischemia-reperfusion model in rats, suggesting inhibitory effects on oxidative injury to the blood-brain barrier (BBB). Additionally, edaravone also prevented rat cortical edema caused by intracortical AA infusion in which free radical production and subsequent oxidative injury to the BBB are involved. With advances in in vivo measurement technology of oxygen radicals, edaravone was shown to inhibit postischemic increases in .OH production and tissue injury in the penumbral or recirculated area in rat cerebral ischemia models. In clinical studies, edaravone improved the core neurologic deficits, activities of daily living, and functional outcome of stroke patients. Furthermore, a study using proton magnetic resonance spectroscopic techniques showed that edaravone preserved N-acetyl-aspartate in stroke patients, a promising neuronal marker in the brain. Further investigation is essential for a better understanding of free radical-mediated cerebral injury during ischemia followed by recirculation. We hope that edaravone represents a promising neuroprotectant for drug therapy in acute cerebral ischemia.
最长约 10秒,即可获得该文献文件

科研通智能强力驱动
Strongly Powered by AbleSci AI
更新
大幅提高文件上传限制,最高150M (2024-4-1)

科研通是完全免费的文献互助平台,具备全网最快的应助速度,最高的求助完成率。 对每一个文献求助,科研通都将尽心尽力,给求助人一个满意的交代。
实时播报
Anna Jenna发布了新的文献求助10
1秒前
英姑应助Anna Jenna采纳,获得10
13秒前
思源应助Simon采纳,获得10
16秒前
22秒前
23秒前
29秒前
Umair发布了新的文献求助10
29秒前
Simon发布了新的文献求助10
32秒前
Akim应助Umair采纳,获得10
38秒前
舒心豪英完成签到 ,获得积分10
50秒前
哭泣青烟完成签到 ,获得积分10
1分钟前
脑洞疼应助远方采纳,获得10
1分钟前
充电宝应助木四点采纳,获得10
1分钟前
Akim应助LPH01采纳,获得30
1分钟前
1分钟前
我是老大应助不安映秋采纳,获得10
1分钟前
sui应助科研通管家采纳,获得10
1分钟前
木四点发布了新的文献求助10
1分钟前
1分钟前
2分钟前
2分钟前
LPH01发布了新的文献求助30
2分钟前
Umair发布了新的文献求助10
2分钟前
2分钟前
汪鸡毛完成签到 ,获得积分10
2分钟前
不安映秋发布了新的文献求助10
2分钟前
2分钟前
李爱国应助Umair采纳,获得10
2分钟前
知性的致远完成签到,获得积分10
2分钟前
2分钟前
思源应助既然采纳,获得10
2分钟前
林非鹿完成签到,获得积分10
2分钟前
夏瑞完成签到 ,获得积分10
2分钟前
3分钟前
慕青应助青儿采纳,获得10
3分钟前
3分钟前
jinyy发布了新的文献求助10
3分钟前
Anna Jenna发布了新的文献求助10
3分钟前
3分钟前
3分钟前
高分求助中
The Young builders of New china : the visit of the delegation of the WFDY to the Chinese People's Republic 1000
юрские динозавры восточного забайкалья 800
English Wealden Fossils 700
Chen Hansheng: China’s Last Romantic Revolutionary 500
宽禁带半导体紫外光电探测器 388
Case Research: The Case Writing Process 300
Global Geological Record of Lake Basins 300
热门求助领域 (近24小时)
化学 医学 生物 材料科学 工程类 有机化学 生物化学 物理 内科学 纳米技术 计算机科学 化学工程 复合材料 基因 遗传学 催化作用 物理化学 免疫学 量子力学 细胞生物学
热门帖子
关注 科研通微信公众号,转发送积分 3142672
求助须知:如何正确求助?哪些是违规求助? 2793563
关于积分的说明 7806899
捐赠科研通 2449789
什么是DOI,文献DOI怎么找? 1303477
科研通“疑难数据库(出版商)”最低求助积分说明 626959
版权声明 601314