新型[^(99m)TcN]^(2+)核含吗啡啉类氨荒酸盐配合物的初步研究

A PRELIMINARY STUDY ON A NEW ^(99m)Tc NITRIDO COMPLEX WITH DITHIOCARBAMATE LIGAND CONTAINING THE MORPHOLINO GROUP

采用了SnCl2.2H2O为还原剂,丁二酰二酰肼(SDH)为N3-离子提供体,在室温下制备[99mTcN]2+中间体,然后与2-(4-吗啡啉代)乙基氨荒酸盐(MPEDTC)发生配体交换反应得到放射化学纯度大于90%的99mTcN-MPEDTC配合物.该配合物是一种体外稳定性良好的脂溶性电中性物质.小鼠体内生物分布结果表明:99mTcN-MPEDTC配合物在小鼠心肌和脑中摄取量均不高,且靶与非靶比值偏低,不适合作为心脑显像剂,为寻求新型心脑显像剂,该配合物的结构需要进一步修饰.

By introducing the morpholino function into dithiocarbamate for the first time, the complex ^99mTcN-MPEDTC（MPEDTC： 2, 4-morpholino ethyl dithiocarbamate） is synthesized through ligand-exchange reaction. The two step procedure involves the initial reaction of 99mTcO^-4 with succinic dihydrazide（SDH） as a donor of nitride nitrogen atom（N^3- ） in the presence of stannous chloride dihydrate as reducing agent, and followed by the addition of the ligand MPEDTC. The radiochemical purity（RCP） of the complex is over 90% as measured by thin layer chromatography（TLC）. The complex is ncutral and lipophilic; and it has good stability at room temperature. Biodistribution results in mice indicate that ^99mTcN-MPEDTC has a low heart and brain uptake and low target/non-target ratios, thus making it unsuitable for cerebral and myocardial imaging. To seek a new good brain and heart imaging agent, the structure of the complex should be modified in the future.