Synthesis and characterization of new99mTc-radiopharmaceuticals with dithiobenzoate derivatives for the study of septic inflammatory processes
作者:F. Mevellec、A. Roucoux、N. Noiret、A. Moisan、H. Patin、A. Duatti
DOI:10.1002/jlcr.673
日期:2003.3.30
Improved methods for the preparation of 99mTc-radiopharmaceuticals containing dithiobenzoate ligands, in sterile and pyrogen free conditions, are described. These procedures are based on the reaction of these ligands either with [99mTc] pertechnetate in the presence of a strong reducing agent (HCl/tertiary phosphine, SnCl2·2H2O), or with pre-reduced complexes obtained from different kit formulations. All the preparations led to the high-yield formation of the neutral and lipophilic 99mTc-complex [99mTc][Tc(S3CPh)2(S2CPh)], which is analogous to the corresponding compounds obtained with rhenium and the long-lived β-emitting isotope technetium-99 g recently described. HPLC analysis and thin layer chromatography were used to confirm the characterisation of the resulting 99mTc-radiopharmaceutical which was found to be potentially suitable for blood-cell labelling as applied to the diagnosis of inflammatory processes. Copyright © 2003 John Wiley & Sons, Ltd.
本文描述了在无菌和无热原条件下制备含二硫苯甲酸配体的99mTc放射性药物的改进方法。这些方法基于这些配体与[99mTc]高锝酸盐在强还原剂(HCl/三烷基膦,SnCl2·2H2O)存在下的反应,或与来自不同试剂盒配方的预还原复合物反应。所有制备过程都高产率地形成了中性且脂溶性的99mTc-复合物[99mTc][Tc(S3CPh)2(S2CPh)],这一复合物与最近报道的铼和长寿命β发射体锝-99g所获得的相应化合物类似。通过HPLC分析和薄层色谱法验证了所得99mTc放射性药物的特性,发现其可能适用于血细胞标记,用于炎症过程的诊断。版权所有 © 2003 John Wiley & Sons, Ltd.