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基于顺磁性钆(III)配合物的创新型磁共振成像诊断剂。

Innovative magnetic resonance imaging diagnostic agents based on paramagnetic Gd(III) complexes.

作者信息

Aime Silvio, Dastrù Walter, Crich Simonetta Geninatti, Gianolio Eliana, Mainero Valentina

机构信息

Dipartimento di Chimica IFM, Università di Torino, via P Giuria 7, 10125 Torino, Italy.

出版信息

Biopolymers. 2002;66(6):419-28. doi: 10.1002/bip.10357.

DOI:10.1002/bip.10357
PMID:12658728
Abstract

Gd(III) complexes are under intense scrutiny as contrast agents for magnetic resonance imaging (MRI). They act by enhancing tissutal proton relaxation rates. Much has already been done in order to get an in-depth understanding of the relationships between structure, dynamics, and contrastographic ability of these paramagnetic complexes. Their potential in the assessment of flow, perfusion, and capillary permeability has already been established. The next challenges are in the field of molecular imaging applications, which would allow the attainment of early diagnosis based on the recognition of specific reporters of the onset of the pathological state. To this end, Gd(III) complexes have to be endowed with improved targeting capabilities by conjugating suitable recognition synthons on their surfaces. Small peptides are candidates of choice for the attainment of this goal. Moreover, the intrinsic low sensitivity of the NMR techniques implies the need to deliver large amounts of contrast agents to the target in order to get its visualization in the resulting images. Highly efficient delivery systems have been identified, which bring a great promise for the development of innovative diagnostic agents based on Gd(III) complexes.

摘要

钆(III)配合物作为磁共振成像(MRI)的造影剂正受到密切关注。它们通过提高组织质子弛豫率来发挥作用。为了深入了解这些顺磁性配合物的结构、动力学和造影能力之间的关系,已经开展了大量工作。它们在评估血流、灌注和毛细血管通透性方面的潜力已经得到证实。接下来的挑战在于分子成像应用领域,这将使基于对病理状态起始的特定报告分子的识别实现早期诊断成为可能。为此,必须通过在钆(III)配合物表面连接合适的识别合成子来赋予其更好的靶向能力。小肽是实现这一目标的首选候选物。此外,核磁共振技术固有的低灵敏度意味着需要向目标输送大量造影剂,以便在所得图像中实现其可视化。已经确定了高效的输送系统,这为基于钆(III)配合物的创新诊断剂的开发带来了巨大希望。

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