Synthesis, metal complexation and biological evaluation of a novel semi-rigid bifunctional chelating agent for ^99mTc labelling

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• 作者：Julien Le Gal ; Sandra Michaud ; Marie Gressier ; Yvon Coulais and Eric Benoist
• 关键词：Radiopharmaceuticals ; Technetium-99m ; Rhenium ; Bifunctional chelating agent ; Metallic complexes
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2006
• 期刊代码：9_09680896
• 类别：ch
• 出版时间：1 May 2006
• 卷：14
• 期：9
• 页码：2904-2909
• 文件大小：139 K

摘要

A novel bifunctional chelating agent bearing an aromatic ring has been synthesised and characterised. This ligand formed well-defined oxorhenium complexes. The analogous ^99mTcO-complex was obtained in an excellent yield with high radiochemical purity (>95%). The biodistribution of the ^99mTc-complex after intravenous injection studied in normal rats showed that the activity was excreted mainly via renal-urinary pathway indicating its use for labelling peptides with ^99mTc.