期刊论文

Xia, J.-Y.

中文

核化学与放射化学

0253-9950

2008

30

2

86-92

国家自然科学基金资助项目（10405034）； 长沙理工大学基金资助项目（1004131）；

本校为第一且通讯机构

选择了3种三齿配体(二(2-吡啶甲基)-胺基)-乙胺(L_1NH_2)、(二(2-吡啶甲基)-氨基)-乙酸(L_2H)和((6-胺基-N-叔丁氧基羰基-己基)-吡啶-2-甲基氨基)-乙酸(L_3NH_2),用于设计合成新的以 fac-[~(188)Re(CO)_3]~+为核心的放射性药物.3种配体在低浓度(10~(-5) mol/L)的条件下,反应时间小于60 min,标记率可达90%以上,放射化学纯度大于92%;3种标记物的体外稳定性均很高,标记后24 h内基本不分解.生物分布结果表明,配合物均能较快地从血液和多数的组织器官中清除,主要通过排泄系统代谢,并初步探讨了这3个配合物在小鼠体内的生物分布行为可能与它们的脂水分配系数lg P有关.lg P值(-0.36)高的配合物[~(188)R...

Three novel tridentate ligands (L1NH2 = bis(2-pyridylmethyl)-amino)-ethylamine, L2H = bis(2-pyridylmethyl)-amino)-acetic acid, L3NH2 = [(6-amino-hexyl)-pyridyl-2-methyl-amino]-acetic acid) were used as bifunctional chelating agents for the organometallic precursor fac-[188Re(CO)3 (H2O)3]+. The results of labeling condition experiments show that a radiochemical purity higher than 92% can be obtained within 60 min by the reaction of fac-[188Re(CO)3]+ core in a condition (pH = 7.4) with a very small amount (10-5 mol/L) of these three ligands. The stability experiments in vitro demonstrate that fa...