地拉卓二盐酸盐

地拉卓二盐酸盐

中文名称地拉卓二盐酸盐
中文同义词地拉卓二盐酸盐;1,4-双[3-(3,4,5-三甲氧基苯甲酰氧基)丙基]高哌嗪二盐酸盐;(1,4-二氮杂环庚烷-1,4-二基)双(丙烷-3,1-二基) 双(3,4,5-三甲氧基苯甲酸酯) 二盐酸盐;盐酸地拉卓
英文名称DILAZEP DIHYDROCHLORIDE
英文同义词DILAZEP DIHYDROCHLORIDE;1,4-BIS[3-(3,4,5-TRIMETHOXYBENZOYLOXY)PROPYL]HOMOPIPERAZINE DIHYDROCHLORIDE;N,N'-BIS[3-(3,4,5-TRIMETHOXY-BENZOYLOXY)PROPYL]HOMOPIPER-AZINE DIHYDROCHLORIDE;1,4-bis(3-(3,4,5-trimethoxybenzoyloxy)-propyl)perhydro-1,4-diazepinedihydroc;astac;astac4898;benzoicacid,3,4,5-trimethoxy-,diesterwithtetrahydro-1h-1,4-diazepine-1,4(5;comelian
CAS号20153-98-4
分子式C31H46Cl2N2O10
分子量677.61
EINECS号243-548-8
相关类别
Mol文件20153-98-4.mol
结构式地拉卓二盐酸盐 结构式

地拉卓二盐酸盐 性质

熔点194-198° (monohydrate)
储存条件2-8°C
溶解度在水中的溶解度10 mg/mL
形态粉末
颜色白色
水溶解性Soluble to 100 mM in water

地拉卓二盐酸盐 用途与合成方法

Dilazep dihydrochloride 是腺苷摄取的抑制剂。Dilazep dihydrochloride 通过增强腺苷的作用而具有脑和冠状血管舒张作用。Dilazep dihydrochloride 还可抑制缺血性损伤,血小板聚集和核苷的膜转运。

Adenosine uptake

The uptake mechanism has been studied extensively in vitro and Dilazep, NBI and Dipyridamole have been reported to inhibit the uptake of adenosine into different cells. Of these compounds, Dilazep and NBI are almost 10 times more potent than Dipyridamole. In addition, only Dilazep is water soluble and no solubility aiding organic solvent is needed for preparing an aqueous solution.

After administration of Dilazep, even low doses (0.04-0.1 mg/kg/min) of exogenous adenosine significantly increases superior mesenteric arterial conductance (SMAC) and elevates arterial plasma adenosine concentration. The increased adenosine levels were highly correlated with the increased percentage of change of SMAC and values for R max and EC 50 were 193.4% change of SMAC and 2.8 μM, respectively. Administration of bolus doses of 8-phenyltheophylline abolishes the ability of Dilazep to potentiate vasodilation, but did not affect isoproterenol-induced relaxation.
Dilazep inhibits the phospholipase activation in reperfused heart mitochondria and also inhibits the lipid peroxidation caused by cerebral ischemia and reperfusion. Dilazep may prevent ischemic cerebral injury due to an increase in cerebral blood flow and/or its protective effects on vascular endothelial cell membrane.

安全信息

危险品标志Xi
危险类别码36/37/38
安全说明26-36
WGK Germany2
RTECS号DI0250000
毒性LD50 in male mice, male rats (mg/kg): 26.6, 19.1 i.v.; 161, 90.1 i.p.; 3740, >2150 orally (Abel)

MSDS信息

提供商 语言
英文

地拉卓二盐酸盐 上下游产品信息

上游原料
"地拉卓二盐酸盐"相关产品信息
3,4-二甲氧基-5-羟基苯甲酸 3,4-二羟基-5-甲氧基苯甲酸甲酯 3,4,5-三甲氧基苯甲酸乙酯 丁香酸 3,4-二羟基苯甲酸乙酯 海索苯定 1-乙基高哌嗪 丁香酸甲酯 3,5-二甲氧基苯甲酸 双酯嗪 3,5-二羟基苯甲酸甲酯 甲基-Β-D-吡喃半乳糖苷 3,4,5-三甲氧基苯甲酸 没食子酸丙酯 3,4,5-三甲氧基苯甲酸甲酯 3,5-二乙氧基基苯甲酸甲酯 3,4-二甲氧基-5-羟基苯甲酸甲酯 高哌嗪
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