A novel organometallic aqua complex of technetium for the labeling of biomolecules:: Synthesis of [99mTc(OH2)3(CO)3]+ from [99mTcO4]- in aqueous solution and its reaction with a bifunctional ligand
A novel organometallic aqua complex of technetium for the labeling of biomolecules:: Synthesis of [99mTc(OH2)3(CO)3]+ from [99mTcO4]- in aqueous solution and its reaction with a bifunctional ligand
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DOI：
10.1021/ja980745t
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发表时间：
1998-08-12
影响因子：
15
通讯作者：
Kaden, TA
中科院分区：
文献类型：
--
作者：
Alberto, R;Schibli, R;Kaden, TA
我们在此提出的水和空气稳定的有机金属水配合物[99 mTc（OH 2）3（CO）3]+直接从[99 mTcO 4]-在盐水中1大气压下的CO的第一个合成。随后取代的不稳定的水配体的双功能配体连接到生物分子，使羰基配合物在生命科学中的一般情况下，特别是在核医学中的引入。有机金属配合物在核医学中的应用（即用于标记受体结合生物分子，如类固醇激素，脑示踪剂等）已在文献中提出。1-4然而，这些方法是基于经典的有机金属合成，因此，常规使用受到缺乏前体的实际制备的影响。放射性核素99 mTc在诊断核医学中是重要的。它价格便宜，在任何医院都很容易买到。因此，它是高优先级的开发有效的标记方法（在产量和配体/金属比方面）的生物分子，衍生与螯合功能的99 mTc中心。迄今为止，已发表的方法主要依赖于用四齿N和S配体稳定Tc（V）。5-8除了这种共轭物的生物活性的不可预测的保留，该方法在大多数情况下需要从冷的，未标记的材料（受体饱和）或从分解产物，如99 mTcO 2的纯化。
We present herein the first synthesis of the water and air stable organometallic aqua complex [99mTc (OH2) 3 (CO) 3]+ directly from [99mTcO4]-in saline under 1 atm of CO. Subsequent substitution of the labile water ligands by a bifunctional ligand attachable to biomolecules enables the introduction of carbonyl complexes in life sciences in general and in nuclear medicine in particular. The application of organometallic complexes in nuclear medicine (ie for the labeling of receptor binding biomolecules like steroid hormones, brain tracers, and others) has been proposed in the literature. 1-4 Those approaches, however, were based on classical organometallic syntheses, and thus, the routine use suffered from the lack of practical preparations of precursors. The radionuclide 99mTc is important in diagnostic nuclear medicine. It is inexpensive and readily available in any hospital. Consequently, it is of high priority to develop efficient labeling methods (in terms of yield and ligand/metal ratio) for biomolecules, derivatized with a chelating function for the 99mTc center. To date, the published methods mostly rely on the stabilization of Tc (V) with tetradentate N and S ligands. 5-8 Besides nonpredictable retention of biological activity of such conjugates, the methods entailed in most cases purification either from cold, unlabeled material (receptor saturation) or from decomposition products such as 99mTcO2.