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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

CAS:103745-39-7
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;
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。 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。
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。

合成路线

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图谱

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1H NMR : Predict


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