新型[^99TcN]^2＋核含吗啡啉类氨荒酸盐配合物的初步研究

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.

A PRELIMINARY STUDY ON A NEW ^99mTc NITRIDO COMPLEX WITH DITHIOCARBAMATE LIGAND CONTAINING THE MORPHOLINO GROUP

By introducing the morpholino function into dithiocarbamate for the first time,the complex(()~(99m)TcN-)MPEDTC(MPEDTC:2,4-morpholino-ethyl dithiocarbamate) is synthesized through ligand-exchange reaction.The two step procedure involves the initial reaction of()~(99m)TcO~-_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 neutral and lipophilic;and it has good stability at room temperature.Biodistribution results in mice indicate that()~(99m)TcN-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.