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20153-98-4

中文名稱 地拉卓二鹽酸鹽
英文名稱 DILAZEP DIHYDROCHLORIDE
CAS 20153-98-4
分子式 C31H46Cl2N2O10
分子量 677.61
MOL 文件 20153-98-4.mol
更新日期 2024/12/23 10:32:54
20153-98-4 結(jié)構(gòu)式 20153-98-4 結(jié)構(gòu)式

基本信息

中文別名
地拉卓二鹽酸鹽
1,4-雙[3-(3,4,5-三甲氧基苯甲酰氧基)丙基]高哌嗪二鹽酸鹽
英文別名
astac
k-285
C12954
C-4898
labitan
comelian
cormelian
astac4898
DILAZEP DIHYDROCHLORIDE
h)dipropanol,dihydrochloride

物理化學性質(zhì)

熔點194-198° (monohydrate)
儲存條件2-8°C
溶解度H2O: 10 mg/mL
溶解度在水中的溶解度10 mg/mL
形態(tài)powder
顏色white
水溶解性溶于水至100mM

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H315-H319-H335
危險品標志Xi
危險類別碼36/37/38
安全說明26-36
WGK Germany2
WGK Germany2
RTECS號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)

常見問題列表

生物活性
Dilazep dihydrochloride 是腺苷攝取的抑制劑。Dilazep dihydrochloride 通過增強腺苷的作用而具有腦和冠狀血管舒張作用。Dilazep dihydrochloride 還可抑制缺血性損傷,血小板聚集和核苷的膜轉(zhuǎn)運。
靶點

Adenosine uptake

體外研究

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.

體內(nèi)研究

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.

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