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为开发作为潜在 pH 敏感 MRI/PET 探针的 Gd(III)-Ga(III) 双位点配合物,正交合成一种杂二聚体配体。

Orthogonal synthesis of a heterodimeric ligand for the development of the Gd(III)-Ga(III) ditopic complex as a potential pH-sensitive MRI/PET probe.

机构信息

Dipartimento di Scienze e Innovazione Tecnologica, Università degli Studi del Piemonte Orientale Amedeo Avogadro, Viale T. Michel 11, I-15121 Alessandria, Italy.

出版信息

Org Biomol Chem. 2013 Feb 13;11(10):1683-90. doi: 10.1039/c2ob27200h.

DOI:10.1039/c2ob27200h
PMID:23360969
Abstract

A heterodimeric polyaminocarboxylate ligand based on a DO3A-sulfonamide linked to AAZTA (6-amino-6-methylperhydro-1,4-diazepinetetracarboxylic acid) was synthesised via an orthogonal pathway in order to differentiate the two chelating cages and allow the formation of a Gd(III)-Ga(III) heteroditopic complex. The goal is to create a smart MRI/PET probe with pH dependent relaxivity and with the bimodal imaging approach that enables direct quantification of the stimulus, in this case pH. A (1)H NMR relaxometric study of the Gd-Ga heteroditopic complex addressed the pH modulation of the relaxivity and thus its possible use as an MRI pH sensitive probe.

摘要

一种基于 DO3A-磺酰胺连接到 AAZTA(6-氨基-6-甲基全氢-1,4-二氮杂环四羧酸)的杂二聚多胺多羧酸配体通过正交途径合成,以区分两个螯合笼,并允许形成 Gd(III)-Ga(III)杂双位络合物。目标是创建一种具有 pH 依赖性弛豫率的智能 MRI/PET 探针,并采用双模态成像方法,能够直接定量刺激,在这种情况下是 pH。对 Gd-Ga 杂双位络合物的 (1)H NMR 弛豫率研究解决了弛豫率的 pH 调节问题,因此它可能被用作 MRI pH 敏感探针。

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