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肝靶向药物研究——模型化合物NGA-去甲替林的合成及其趋肝性
99mTc-NGA-NORTRIPTYLINE AS A MODEL COMPOUND OF HEPATIC TARGETING DRUGS:PREPARATION AND RESEARCH ON LIVERTAXIS
【摘要】 肝细胞膜上的肝结合蛋白(HBP)是无唾液酸糖蛋白的受体。作者合成了无唾液酸糖蛋白的类似物—半乳糖新糖白蛋白(NGA)并用其作为肝靶向药物的载体,采用琥珀酸酐法与药物去甲替林(NT)偶联得NGA-NT。以此作模型化合物,经99mTc标记后的动物放射显像及HPLC检测结果,说明NGA-NT在血中稳定,在肝脏降解释出NT,具有显著的趋肝性。
【Abstract】 Galactosyl-neoglycoalbumin(NGA) is a special ligand of asialoglycoprotein receptor which exists in the human liver. We used NGA as a carrier of hepatic targeting drugs and prepared a couple of NGA with Nortriptylin(NT) by succinyl bridge. The model compound was labelled with 99mTc. The radionuclide image showed that the 99mTc-NGA-NT had remarkable livertaxis.The result of HPLC revealed that the NGA-NT was stable in blood and released NT at the livers in tested rabbits.
【关键词】 无唾液酸糖蛋白受体;
半乳糖新糖蛋白;
肝靶向药物;
【Key words】 Asialoglycoprotein receptor; Galactosyl-Neoglycoalbamin(NGA); Hepatic targeting drugs;
【Key words】 Asialoglycoprotein receptor; Galactosyl-Neoglycoalbamin(NGA); Hepatic targeting drugs;
【基金】 卫生部科学研究项目基金
- 【文献出处】 中国药物化学杂志 ,Chinese Journal of Medicinal Chemistry , 编辑部邮箱 ,1992年02期
- 【被引频次】3
- 【下载频次】85