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1,4,7,10-四氮杂环十二烷-1,4,7-三乙酸(DO3A)-乙氧基苄基(EOB)轭合物钆配合物作为新型大环肝胆磁共振成像对比剂。

Gadolinium Complex of 1,4,7,10-Tetraazacyclododecane-1,4,7-trisacetic Acid (DO3A)-Ethoxybenzyl (EOB) Conjugate as a New Macrocyclic Hepatobiliary MRI Contrast Agent.

机构信息

Laboratory Animal Center, Daegu-Gyeongbuk Medical Innovation Foundation Chumbok-ro 80, Dong-gu, Daegu 41061, Korea.

出版信息

J Med Chem. 2017 Jun 22;60(12):4861-4868. doi: 10.1021/acs.jmedchem.7b00060. Epub 2017 May 31.

Abstract

We report the synthesis of a macrocyclic Gd chelate based on a 1,4,7,10-tetraazacyclododecane-1,4,7-trisacetic acid (DO3A) coordinationn cage bearing an ethoxybenzyl (EOB) moiety and discuss its use as a T hepatobiliary magnetic resonance imaging (MRI) contrast agent. The new macrocyclic liver agent shows high chelation stability and high r relaxivity compared with linear-type Gd chelates, which are the current clinically approved liver agents. Our macrocyclic, liver-specific Gd chelate was evaluated in vivo through biodistribution analysis and liver MRI, which demonstrated its high tumor detection sensitivity and suggested that the new Gd complex is a promising contrast agent for liver cancer imaging.

摘要

我们报告了一种基于 1,4,7,10-四氮杂环十二烷-1,4,7-三乙酸(DO3A)配位笼的大环 Gd 螯合物的合成,该配位笼带有乙氧基苄基(EOB)部分,并讨论了其作为 T1 肝胆磁共振成像(MRI)造影剂的用途。与当前临床批准的肝造影剂相比,新型大环肝造影剂具有更高的螯合稳定性和 r1 弛豫率。我们的大环、肝特异性 Gd 螯合物通过体内分布分析和肝 MRI 进行了评估,结果表明其具有高肿瘤检测灵敏度,并表明新型 Gd 配合物是一种有前途的肝癌成像造影剂。

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