化合物简介
A potent calcium antagonist vasodilator which is considered to act by employing different mechanisms from the usual calcium channel blockers since it inhibits (1) calcium ionophore A23187 induced contraction in arterial strips and (2) phenylephrine induced contraction in calcium free media suggesting that its site of action is in the intracellular space. Also reported to potently inhibit Rho-associated Kinase (ROCK IC50= 10.7 uM).
基本信息
中文名称
法舒地尔
英文名称
FASUDIL
中文别名
1-(5-硫代异喹啉)哌嗪二盐酸盐、六氢-1-(5-异喹啉基磺酰基)-1H-1,4-二氮卓
英文别名
Fasudilum、Fasudilum [inn-latin]、H-1077 dihydrochloride、hexahydro-1-(5-isoquinolinylsulfonyl)-1H-1,4-diazepine、at877、HA-1077 DIHYDROCHLORIDE NOVEL VASODILATO R AGE、1-(5-isoquinolinesulphonyl)-homopiperazine、HA 1077,DIHYDROCHLORIDE、1-(5-Isoquinolinesulfonyl)-1H-hexahydro-1,4-diazepine,Dihydrochloride、1-(5-ISOQUINOLINE-SULFONYL)-HOMOPIPERAZINE
CAS号
103745-39-7
分子式
C14H19Cl2N3O2S
分子量
364.291
精确质量
363.058
PSA
70.68
LOGP
4.1703
编号系统
PubChem号
24895456
RTECS号
HM4031166
MDL号
MFCD00153805
物化性质
外观与性状
白色结晶固体
密度
1.289g/cm3
沸点
506.2ºC at 760mmHg
闪点
259.9ºC
蒸汽压
2.55E-12mmHg at 25°C
安全信息
RTECS号
HM4031166
WGK Germany
3
海关编码
2933990090
生产方法及用途
生产方法
异喹啉经发烟硫酸磺化，生成的磺酸转化为磺酰氯，再和二氮革反应，得到产物。
用途
钙拮抗剂。用于蛛网膜下出血手术后的血管痉挛，也可用于神经保护、急性脑动脉栓塞、慢性脑梗死和心绞痛。
