[^(188)Re(CO)_3(H_2O)_3]^+标记用双功能联接剂的制备、标记及性质

Preparation of Several Bifunctional Chelating Agents for Precursor [^(188)Re(CO)_3(H_2O)_3]^+ and Their Radiolabelation and Characteration

合成了几个具有代表性的适于[188Re(CO)3(H2O)3]+标记用的双功能联接剂分子,并对其羰基铼的标记条件进行了优化。结果表明:在最优条件下,上述标记物的放化纯均大于95%。放置实验和体外竞争实验表明:标记物皆有很好的稳定性,在48 h内,放化纯无明显改变。该类分子有望用于生物活性分子羰基铼标记工作中。

Several representative bifunctional chelating agents （BFCA） molecules which can coordinate with [Re（CO）3 （H2 O）3]＋ were synthesized. On the NCA level, the ligands allow labelling yields 〉 95 % with [^188 Re （CO）3 （H2O）3 ]＋ under mild reaction conditions. Incubation of the corresponding ^188Re complexes in PBS buffer and human serum at 37 ℃ reveals good stabilities. Decomposition product is main ^188ReO/. The routine kit-preparation of the precursor [^188 Re （CO）3 （H2O）3 ]＋ in combination with tailor-made ligand systems enables the organometallic labelling of biomolecules with unprecedented high specific activities.