99Tcm(CO)3-PNP5的合成及初步生物分布

采用两步法制备了99Tcm(CO)3-N,N-二[二(3-甲氧基丙基)膦基乙基]-2-乙氧基乙胺(99Tcm(CO)3-PNP5)新型配合物,标记率和放化纯度均大于90%。理化性质研究表明:99Tcm(CO)3-PNP5是一种体外稳定性好、具有一定脂溶性的阳离子配合物。小鼠生物分布研究表明,99Tcm(CO)3-PNP5在心肌中有一定的初始摄取和较好的滞留;血和肺的初始摄取较低,清除较快;肝中的初始摄取高,而清除迅速。在配合物中引入Tween-80后,配合物在小鼠体内心肌初始摄取明显升高,滞留也较好;肝中初始摄取较低且清除很快,心与肝的放射性摄取比(T/NT)高,说明Tween-80的引入明显改善了配合物99Tcm(CO)3-PNP5的生物性能。

Synthesize and Preliminary Biodistribution of 99Tcm(CO)3-PNP5

99Tcm(CO)3-PNP5(PNP5: bis(dimethoxypropylphosphinoethyl)ethoxyethylamine) is synthesized through a simple two-step procedure by ligand exchange reaction and its biological characters are studied.Labelling conditions of 99Tcm(CO)3-PNP5 are optimized.Its labelling yield and radio chemical purity are all over 90% determined by TLC.The results of partition coefficient,charge character and stability studies indicate that 99Tcm(CO)3-PNP5 is a lipophilic cation ligand with complex with positiue charge and good stability.Biological properties of 99Tcm(CO)3-PNP5 and 99Tcm(CO)3-PNP5(T)(adding Tween) are valued contrastively in mice.The results show that 99Tcm(CO)3-PNP5(T) have higher myocardial uptake,lower liver uptake,and higher heart-to-liver ratio.It indicats that the biological properties of 99Tcm(CO)3-PNP5 are improved obviously by adding Tween-80.