含生物素的双功能螯合剂合成及99Tcm(CO)3(H2O)3+标记
Bifunctional Chelate for Radiolabeling of Biotin With99Tcm(CO)3(H2O)3+
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摘要: 设计合成了一种新的用于生物素偶联的双功能螯合剂N-α-(2-皮考基)-N-ε-D-生物素基-L-赖氨酸甲酯( PLB )，并完成其Re(CO)3PLB配合物的合成及化学结构的表征。99Tc m(CO)3(H2O)3+ 的标记条件研究表明，PLB配体浓度在10μmol/L以上，pH在正常生理值7.4左右，于95℃加热30min，标记物的放化纯度大于95％，比活度达37～55.5TBq/mmol。
Abstract: A novel tridentate ligand for Re /99Tcm(CO)3(H2O)3+ core, coupled with biotin, is designed and synthesized. Radiolabeling of PLB ligand (PLB =N-α-(2-picolyl)-N-ε-biotinyl-L-lysine methyl ester) with 99Tcm(CO)3(H2O)3+ precursor is carefully investigated, and more than 95% of yield is achieved under optimized condition.
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