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基于季胺基修饰的核磁共振成像造影剂的合成
引用本文:王伟,汤伟军,郝士婧,陈莹莹,胡爱国. 基于季胺基修饰的核磁共振成像造影剂的合成[J]. 医学教育探索, 2013, 0(5): 523-528
作者姓名:王伟  汤伟军  郝士婧  陈莹莹  胡爱国
作者单位:华东理工大学材料科学与工程学院,上海市先进聚合物材料重点实验室,上海 200237;复旦大学附属华山医院放射科,上海 200040;华东理工大学材料科学与工程学院,上海市先进聚合物材料重点实验室,上海 200237;华东理工大学材料科学与工程学院,上海市先进聚合物材料重点实验室,上海 200237;华东理工大学材料科学与工程学院,上海市先进聚合物材料重点实验室,上海 200237
基金项目:国家自然科学基金(21274042)
摘    要:
利用季胺基团具有高水溶性的特点,合成了一种水溶性良好且带有长烷烃链的核磁共振成像造影剂。通过在1,4,7,10 四氮杂环十二烷(cyclen)的骨架碳原子上引入季胺基团,并分别对4个仲氨基进行亲电取代,得到具有季胺基侧链的多齿配体;在不影响对钆(Ⅲ)离子的络合能力的同时,提高了配合物的弛豫率,并赋予其良好的水溶性。长烷烃链和季胺基团的同时引入为该类配合物的进一步功能化提供了可能性。

关 键 词:核磁共振成像; 造影剂; 季胺基; 长链烷烃
收稿时间:2013-04-16

Synthesis of Magnetic Resonance Imaging Contrast Agent with Tethered Quaternary Ammonium Group
WANG Wei,TANG Wei-jun,HAO Shi-jing,CHEN Ying-ying and HU Ai-guo. Synthesis of Magnetic Resonance Imaging Contrast Agent with Tethered Quaternary Ammonium Group[J]. Researches in Medical Education, 2013, 0(5): 523-528
Authors:WANG Wei  TANG Wei-jun  HAO Shi-jing  CHEN Ying-ying  HU Ai-guo
Affiliation:Shanghai Key Laboratory of Advanced Polymeric Materials, School of Materials Science and Engineering, East China University of Science and Technology, Shanghai 200237, China;Department of Radiology, Huashan Hospital Affiliated to Fudan University, Shanghai 200040, China;Shanghai Key Laboratory of Advanced Polymeric Materials, School of Materials Science and Engineering, East China University of Science and Technology, Shanghai 200237, China;Shanghai Key Laboratory of Advanced Polymeric Materials, School of Materials Science and Engineering, East China University of Science and Technology, Shanghai 200237, China;Shanghai Key Laboratory of Advanced Polymeric Materials, School of Materials Science and Engineering, East China University of Science and Technology, Shanghai 200237, China
Abstract:
Benefited with the high water solubility of quaternary ammonium group, a magnetic resonance imaging (MRI) contrast agent with tethered quaternary ammonium group linked by long alkyl chain was synthesized. The quaternary ammonium group was introduced in the skeleton of 1,4,7,10 tetraazacyclododecane (cyclen), and four secondary amino groups in cyclen were functionalized with carboxymethyl groups, forming a polychelating ligand with a quaternary ammonium side chain. Without affecting the conjugation ability, this ligand forms stable Gd(III) complex showing higher relaxivity than Gd(III) DOTA. With both quaternary ammonium group and long alkyl chain installed in the same molecule, further functionalization or modification to achieve high performance MRI contrast agents is promising.
Keywords:MRI   contrast agent   quaternary ammonium group   long alkane chain
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