99Tcm-MAG3-isoDGR-2C分子探针的制备与体内分布的实验研究

Labeling MAG3-isoDGR-2C with 99Tcm and its biodistribution in mice

目的 摸索99Tcm-MAG3-isoDGR-2C分子探针的标记条件并研究其在正常昆明小鼠体内的生物学分布.方法 利用葡庚糖酸盐（GH）转换络合法进行标记,即首先用99Tcm标记GH形成99TcmO-GH中间体,再进行99Tcm-MAG3-isoDGR-2C的标记;考察pH值和温度等因素对标记率的影响,采用高效液相色谱法鉴定标记物的放射化学纯度;取30只昆明小鼠随机分成6组,分另于注射99cm-MAG3-isoDGR-2C 15、30、60、120、240和360 min后测定其在小鼠体内的分布情况.结果 pH值为4.6、反应温度为100℃时的标记率最高（94.2％）.体内分布研究显示该标记物能够较快地从血液中清除,且心、肺、脾、胃、骨等组织的放射性摄取均很少.结论 99Tcm-MAG3-isoDGR-2C标记率高、血液清除快,具备一定的成为SPECT显像剂的条件.

Objective To analyze the feasibility of labeling MAG3-isoDGR-2C with 99Tcm and investigate the biodistribution of the tracer in normal mice.Methods Glucoheptonate was initially labeled with 99Tcm as the intermediate,followed by MAG3-isoDGR-2C.High-performance liquid chromatography was employed to determine the radiochemical purity.The biodistribution of 99Tcm-MAG3-isoDGR-2C was studied at 15,30,60,120,240 and 360 min after caudal vein injection in normal mice.Results MAG3-isoDGR-2C was successfully labeled with 99Fcm,and the radiochemical purity was 94.2%.The biodistribution revealed that the tracer was rapidly cleared out from the blood with mild activity in the heart,lung,spleen,stomach,and bone.Conclusions MAG3-isoDGR-2C was labeled with 99Tcm with high radiochemical purity,and the tracer could be cleared out quickly.Therefore,MAG3-isoDGR-2C is a potential molecular tracer in the study of early cancer diagnosis.