以含吡啶环的化合物[二(2-吡啶甲基)-氨基]-乙酸(H^2L)为双功能螯合剂,使用fac-[^188Re(CO)3(H2O)3]^+间接标记人血清白蛋白(IgG),为fac-[^188Re(CO)3(H2O)3]^+标记蛋白或单抗寻找新方法。Fac-[^188Re(CO)3(H2O)3]^+标记条件研究表明,以活泼酯^188Re(CO)3-L^2H-TFP(TFP,2,3,5,6-四氟酚)间接标记IgG时,标记率大于82%。在生理盐水和小牛血清中,48h后产物的放化纯度均大于90%;以fac-[^188Re(CO)3(H2O)3]^+直接标记IgG作对比,标记率仅60%。在生理盐水和小牛血清中,48h后产物的放化纯度〈60%。总的说来,使用fac-[^188Re(CO)3(H2O)3]^+间接标记生物分子时,具有对称结构的含吡啶环的化合物H^2L是潜在的双功能螯合剂。
It is a novel method forfac-[^188Re(CO)3(H2O)3]^+ to radiolabel albumin human serum (IgG) indirectly by the pyridyl-containing bis(2-pyridylmethyl)-amino)-acetic acid (L^2H). The results show that radiolabeling efficiency of IgG with ^188Re(CO)3-L^2H-TFP active ester can be higher than 82% under optimized condition. We studied also the labeling stability over 48 h at 37℃ in 0.9% NaCl or bovine serum albumin with both the labeled products. And it shows that the indirect labeling product (90%) has higher radiochemical purity than the direct labeling product (60%). In summary, the symmetric pyridyl-containing tridentate ligand HEL is a potent bifunctional chelator for the future biomolecules labeling of fac-[^188Re(CO)3(H2O)3]^+.