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为了寻找新的具有亲心肌性质的99mTcN药物,合成了一种新的N2S2配体:N,N’-二(2-巯基丙基)-1,2-苯二胺(BMPBDA)。以SnCl2为还原剂, H2NNH-(C=S)-SCH3为N3-给予体,通过交换反应制备了放化纯大于90%的99mTcN-BMPBDA。探讨了pH值对99mTcN-BMPBDA放化纯的影响,并对其小鼠生物分布进行了研究。结果表明,99mTcN-BMPBDA在心肌中具有较高的初始摄取,静脉注射后2min时的心肌摄取为24.53%ID·g-1。但心肌清除稍快,注射后30min时的心肌摄取为7.97%ID·g-1。血清除较快,血半清除期小于15min,但血液中活性较高。本工作对于设计新的99mTcN心肌显像剂具有参考价值。
In order to find new 99mTcN drug with cardiac muscle properties, a novel N2S2 ligand was synthesized: N, N’-bis (2-mercaptopropyl) -1,2-phenylenediamine (BMPBDA). Using SnCl2 as reductant and H2NNH- (C = S) -SCH3 as the N3-donor, 99mTcN-BMPBDA with more than 90% pure radioactivity was prepared by the exchange reaction. The effect of pH value on the radiochemical purity of 99mTcN-BMPBDA was investigated. The biodistribution of the 99mTcN-BMPBDA was studied. The results showed that 99mTcN-BMPBDA had a higher initial uptake in myocardium, and myocardial uptake was 24.53% ID · g-1 at 2 min after intravenous injection. However, myocardial clearance was slightly faster and myocardial uptake was 7.97% ID · g-1 at 30 min after injection. Serum in addition to faster, half-blood clearance less than 15min, but higher blood activity. This work for the design of a new 99mTcN myocardial imaging agent has a reference value.