Kono A, Maeda T, Karube Y, Shiokawa H, Matsushima Y
J Nucl Med. 1979 Jan;20(1):39-44.
In order to obtain a technetium-99m-labeled cholescintigraphic agent suitable for kit preparation, reactions of a variety of aromatic aldehydes, amino acids, and [99mTc] pertechnetate were examined under mild conditions. Aqueous solutions of the three reactants were heated in a boiling-water bath and the products analyzed by means of thin-layer chromatography for the formation of organic technetium complexes. 3-Hydroxy-4-formylpyridine (HFP) and 1-methyl-3-hydroxy-4-formylpyridinium chloride (N-Me-HFP) formed the complex with excellent yields, whereas 3-hydroxy-2-formylpyridine, 4-nitrosalicylaldehyde, salicylaldehyde, and isonicotinaldehyde did not. The complex is concluded to be the Tc-99m chelate of the Schiff base formed from the aldehyde and amino acbbits administered with the complex of HFP, glutamic acid and Tc-99m. The results indicate that it is promising as a cholescintigraphic agent.
为了获得一种适合制成试剂盒的锝-99m标记的胆闪烁显像剂,在温和条件下考察了多种芳香醛、氨基酸与高锝[99mTc]酸盐的反应。将三种反应物的水溶液在沸水浴中加热,并用薄层色谱法分析产物,以确定有机锝配合物的形成情况。3-羟基-4-甲酰基吡啶(HFP)和1-甲基-3-羟基-4-甲酰基吡啶氯化物(N-Me-HFP)能以优异的产率形成配合物,而3-羟基-2-甲酰基吡啶、4-亚硝基水杨醛、水杨醛和异烟醛则不能。该配合物被认为是由醛与氨基酸形成的席夫碱的Tc-99m螯合物,该氨基酸与HFP、谷氨酸和Tc-99m的配合物一起给药。结果表明,它有望成为一种胆闪烁显像剂。