An exploratory research of new cerebroprotective agents

据估计，日本有150万名脑血管疾病（CVD）患者，其中脑缺血（中风）占CVD的60%以上。最近的数据还显示，心血管疾病的死亡率正在下降，但患者数量没有减少，治疗选择仍然有限。脑缺血/再灌注过程中产生的活性氧和其他游离自由基是神经元细胞损伤的重要介质。依达拉奉是一种根治性清除剂，已被证明对中风患者有效，并在日本临床使用。然而，由于副作用，如肾毒性，依达拉奉的应用受到限制。为了开发新的脑缺血再灌注损伤治疗剂，对新合成的GR103691衍生物进行了新的脑保护剂探索。本研究最重要的结果是发现了一些治疗损伤的有益化合物，这些化合物比依达拉奉更有效。

It is estimated that there are 1,500,000 patients with cerebrovascular disease (CVD) and that cerebral ischemia (stroke) is responsible for more than 60% of CVD in Japan. Recent data also shows that the mortality rate due to CVD is decreasing, however number of patients do not decrease, and therapeutic options is still limited. Reactive oxygen species and other free ragicals generated during cerebral ischemia/reperfusion are critical mediators of neuronal cell damage. Edaravone, a radical scavenger, has been shown to be effective for stroke patients and is clinically used in Japan. However, adoption of edaravone is limited because of side effects, such as renal toxicity.Aim to develop of new therapeutic agents for ischemia/reperfusion injury, new cerebroprotective agents were explored in newly synthetic GR103691 derivatives. The most important results in this study is finding of some useful compounds for the injury and these compounds were more effective than edaravone.