高等学校化学学报 ›› 1997, Vol. 18 ›› Issue (7): 1072.

• 论文 • 上一篇    下一篇

肝靶向性磁共振成像造影剂──含D-半乳糖基的DTPA双酰胺钆配合物的研究

傅雁军, 卓仁禧   

  1. 武汉大学化学系, 国家教育委员会生物医用高分子材料开放实验室, 武汉 430072
  • 收稿日期:1997-02-05 出版日期:1997-07-24 发布日期:1997-07-24
  • 通讯作者: 卓仁禧.
  • 作者简介:傅雁军, 男, 26岁, 博士研究生.
  • 基金资助:

    国家教育委员会博士点基金

Studies on D-Galactose-containing DTPA Bisamide Gadolinium Complexes as Liver-targeting MRI Contrast Agents

FU Yan-Jun, ZHUO Ren-Xi   

  1. Department of Chemistry, Laboratory of Biomedical Polymer Materials of the State EducationCommission of China, Wuhan University, Wuhan 430072
  • Received:1997-02-05 Online:1997-07-24 Published:1997-07-24

摘要: 通过二乙三胺五乙酸的双N-羟基琥珀酰亚胺活性酯与含氨基的乳糖或D-半乳糖衍生物反应,合成了8种含有D-半乳糖基的二乙三胺五乙酸非离子型配体,并进一步合成了其钆(Ⅲ)配合物. 配体及配合物的结构经IR、1HNMR与元素分析表征,对配合物的体外弛豫性能和小鼠急性毒性作了初步研究. 家兔的磁共振成像实验表明这类造影剂具有肝靶向的特性.

关键词: 磁共振成像造影剂, D-半乳糖基, 弛豫性能, 急性毒性, 肝靶向性

Abstract: New lactose-or D-galactose-containing diethylenetriaminepentaacetic acidbisamide ligands and their gadolinium complexes were synthesized by the reaction of bis(N-hydroxysuccinimide ester)of diethylenetriaminepentaacetic acid with amino-containing lac-tose or D-galactose derivatives.Chemical structures of ligands and Gd complexes were char-acterized.In vitro spin-lattice relaxivity and acute toxicity in mice of the complexes havebeen preliminarily investigated.Magnetic Resonance lmaging for rabbit shows that the con-trast agent bearing galactose could be targeted to the liver.

Key words: MRI contrast agents, D-Galactopyranosyl group, Relaxivity, Acute toxicity, Liver-targeting

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