DiethylcarbamazineCitrate

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Chemical Structure| 1642-54-2 同义名 : 枸橼酸乙胺嗪 ;Diethylcarbamazine(citrate)
CAS号 : 1642-54-2
货号 : A553770
分子式 : C16H29N3O8
纯度 : 98%
分子量 : 391.42
MDL号 : MFCD00039124
存储条件:

Pure form Inert atmosphere, room temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Diethylcarbamazine citrate is an inhibitor of arachidonic acid metabolism in filarial microfilaria; is highly specific for several parasites and does not contain any toxic metallic elements[2]. Diethylcarbamazine citrate (DEC) is also anti-inflammatory drug. The only effective anti-inflammatory dose was 50mg/kg to reduce the high levels of glucose, insulin and triglycerides in serum. DEC was not anti-obesity drug because the weights of body, liver and adipose tissues were not changed. In addition, the activity of COX (cyclooxygenase) in DEC treatment decreased significantly, while NF-κBp65 localization in nuclear extracts was obviously inhibited in 50mg/kg treated group[3]. Within 10 s of an intravenous injection of DECC(diethylcarbamazine citrate) (2.5 to 10 mg/kg) there was hypotension, bradycardia and there were reductions in left ventricular and carotid artery dP/dt max. DECC (5 or 10 mg/kg) significantly inhibited prostaglandin F2alpha-induced increases in peak inspiratory intra-tracheal pressure without modifying its pulmonary hypertensive effect[4]. The effect of S. equina ES (excretory-secretory) as antioxidant against rat HCC (hepatocellular carcinoma ), while DEC could modulate such effect when combined with it[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01905423 - Completed - Indonesia ... 展开 >> University of Indonesia, Department of Parasitology Jakarta, Java, Indonesia, 10430 收起 <<
NCT01905423 - Completed - -
NCT03676140 Trachoma Yaws... 展开 >> Lymphatic Filariases Scabies Strongyloidiasis 收起 << Phase 3 Not yet recruiting January 2019 -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.55mL

0.51mL

0.26mL

12.77mL

2.55mL

1.28mL

25.55mL

5.11mL

2.55mL

参考文献

[1]El-Shahawi GA, Abdel-Latif M, et al. Setaria equina: in vivo effect of diethylcarbamazine citrate on microfilariae in albino rats. Exp Parasitol. 2010 Dec;126(4):603-10.

[2]El-Shahawi GA, Abdel-Latif M, Saad AH, Bahgat M. Setaria equina: in vivo effect of diethylcarbamazine citrate on microfilariae in albino rats. Exp Parasitol. 2010;126(4):603‐610

[3]Abdel-Latif M. Diethylcarbamazine citrate ameliorates insulin resistance in high-fat diet-induced obese mice via modulation of adipose tissue inflammation. Int Immunopharmacol. 2015;29(2):607‐612

[4]Abaitey AK, Parratt JR. Cardiovascular effects of diethylcarbamazine citrate. Br J Pharmacol. 1976;56(2):219‐227. doi:10.1111/j.1476-5381.1976.tb07445.x

[5]Abdel-Latif M, Sakran T, El-Shahawi G, El-Fayoumi H, El-Mallah AM. Effect of diethylcarbamazine citrate and Setaria equina excretory-secretory material on rat hepatocellular carcinoma. Arch Immunol Ther Exp (Warsz). 2014;62(6):511‐520