Fasudil
(Synonyms:法舒地尔;盐酸法舒地尔;六氢-1-(5-异喹啉基磺酰基)-1H-1,4-二氮卓;4-(甲氧基甲基)苯乙酸;1-(5-硫代异喹啉)哌嗪二盐酸盐;六氢-1-(5-异喹啉磺酰基)-1H-1,4-二氮杂卓)
目录号 : KG10712
CAS No. : 103745-39-7
纯度 : 98%
Ki: 0.33 μM for ROCK-II
Cerebral vasospasm occurs frequently after subarachnoid hemorrhage (SAH) secondary to rupture of an intracranial aneurysm. The possibility that calcium entry blockers may be effective on a delayed cerebral vasospasm and the effectiveness of intrathecal administration of the calcium antagonist nifedipine and its analog nimodipine on a vasospasm has been shown from a clinical point of view. Fasudil is a class of calcium antagonists different from the calcium entry blockers.
In vitro: The inhibitory effects of fasudil on contractile responses to various agonists were examined on strips of rabbit aorta. The concentration-response curves to 5-hydroxytryptamine, prostaglandin F2alpha, histamine, angiotensin II, noradrenaline and dopamine were concentration-dependently shifted to the right in the presence of fasudil .
In vivo: Intra-coronary administration of fasudil to dog dose-dependently increased coronary blood flow, with no effect on mean blood pressure or heart rate. Intra-coronary infusion of atropine, diphenhydramine or propranolol did not modify the in vivo coronary vasodilator response to fasudil .
Clinical trial: The previous results suggested that fasudil was equally or more effective than nimodipine for the prevention of cerebral vasospasm and subsequent ischemic injury in patients undergoing surgery for SHA .
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分子式 |
C14H17N3O2S
|
分子量 |
291.37
|
CAS号 |
103745-39-7
|
中文名称 |
法舒地尔
|
储存方式 |
Store at -20°C
|