新的心肌显像剂~(113m)In-BAT系列配合物的研究—配体合成、配合物晶体结构及动物分布

    STUDY OF NEW ~(113m)In-BAT COMPLEXES FOR MYOCARDIAL IMAGING AGENTS——SYNTHESIS OF LIGANDS. CRYSTAL STRUCTURE AND BIODISTRIBUTION

    • 摘要: 本文合成出九种新的BAT(双-氨基乙硫醇)类衍生物,并研究~(113m)In-BAT系列配合物的动物分布,得到心肌吸取量与配合物脂溶性之间的定量关系。实验表明,配合物B的心/血、心/肺比值高,是最有希望的心肌显像剂。此外,还首次测得了BAT-TE配体及In-BAT-TE和In-BAT-ETE两种配合物的晶体结构。

       

      Abstract: In this paper, some new BAT derivatives are designed and synthesized in order to find some ideal myocardial imaging agents. These ligands form penta-coordinated complexes with indium cation. The structures of ligand BAT-TE and complexes In-BAT-TE and In-BAT-ETE are determined by X-ray crystallography at first. Biodistribution shows that the higher lipophilicity of complex induces apparently higher myocardial accumulation. Up to date, complex B is the best 113mIn-labeled myocardial imaging agent. It is also suited to 111In.

       

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