An exploratory research of new cerebroprotective agents

据估计，在日本有1，500，000名脑血管疾病（CVD）患者，脑缺血（中风）是造成60%以上CVD的原因。最近的数据还显示，由于CVD的死亡率正在下降，但患者数量并没有减少，治疗选择仍然有限。脑缺血/再灌注过程中产生的活性氧等自由基是神经细胞损伤的重要介质。依达拉奉是一种自由基清除剂，已被证明对中风患者有效，并在日本临床使用。为了开发新的缺血/再灌注损伤的治疗药物，本研究在新合成的GR 103691衍生物中探索新的缺血/再灌注损伤保护剂。本研究的最重要的结果是发现了一些对损伤有效的化合物，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.