蛋白リン酸化酵素阻害剤:塩酸ファスジル(エリル〓)の創製
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概要
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A series of isoquinolinesulfonamide derivatives were synthesized and shown to possess vasodilatory action. 1- (5-Isoquinolinesulfonyl) homopiperazine hydrochloride (fasudil) had more potent vasodilatory effect to vertebral artery than diltiazem. Fasudil inhibits protein kinase and dilates spastic cerebral arteries in the canine two-hemorrhage model. In clinical studies with fasudil administered by intravenous injection in patients who had undergone sugery for subarachnoid hemorrhage, fasudil significantly reduced the occurrence of vasospasm. In Japan, fasudil was approved in june, 1995.
- 社団法人 有機合成化学協会の論文
- 1996-09-01