Two kinds of dinuclear gadolinium-containing magnetic resonance imaging contrast agents and their preparation and application

Abstract

The invention relates to the field of magnetic resonance imaging (MRI), and specifically relates to two dual-core gadolinium-containing magnetic resonance imaging (MRI) contrast agents and preparation and applications thereof. Two contrast agents are obtained by the following steps: respectively connecting two DOTA-NHNH2 groups to two aldehyde groups, and then chelating the DOTA-NHNH2 groups with a paramagnetic metal ion Gd<3+>. The structure of two contrast agents is represented in the description. The gadolinium-containing MRI contrast agents are nonionic and contain phenyl substituents. The lipophilic property of the contrast agents is enhanced due to introduced hydrophobic groups. The contrast agents have selectivity on liver imaging. The total relaxation efficiencies of two contrast agents reach 17.3 mM<-1>S<-1> and 11.1 mM<-1>S<-1>.

Description

technical field [0001] The invention relates to the field of magnetic resonance imaging, in particular to two dinuclear gadolinium-containing magnetic resonance imaging contrast agents and their preparation and application. Background technique [0002] Since Lauterbur realized Magnetic Resonance Imaging (MRI) for the first time in 1973, MRI technology has been highly valued by the scientific community for its non-invasive, painless, precise positioning and image display similar to anatomical maps. The medical field continues to expand and has become one of the most important medical imaging equipment in imaging examinations. However, the resolution of magnetic resonance imaging cannot meet the clinical requirements in some cases. In order to enhance the imaging effect, it is necessary to give magnetic resonance contrast agent before the magnetic resonance examination. According to literature reports, in current clinical MRI, more than 35% of MRI examinations require the us...

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Problems solved by technology

[0005] The purpose of the present invention is to solve the relatively poor thermodynamic stability and dynamic stability of chain molecular contrast agents in the prior art, which are more likely to cause nephrogenic systemic fibrosis in some patients and the occurrence of gadolinium ions in the patient's brain. The problem of deposition, at the same time, is also to solve the problem that most of the contrast agents in the prior art have no organ targeting, so as to provide two less toxic circular molecular contrasts with organ targeting, especially liver targeting Agents and their preparation methods

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