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北京师范大学,北京,100875
Published:01 May 1999
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[1]苗玉斌,何千舸,刘伯里.心肌显像剂~(99m)TcN-BMPBDA的制备及动物体内分布研究[J].核技术,1999(05):271-274.
MIAO Yubin, HE Qiange, LIU Boli. Preparaion and prelminary biodistribution in mice of 99mTcN-BMPBDA for myocardial perfusion imaging[J]. Nuclear techniques, 1999, (5): 271-274.
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 complexes for myocardial perfusion imaging
a new N2S2 ligand of N
N’-bis(2-mercapto-propyl)- 1
2-benzenediamine (BMPBDA) has been synthesized and its 99mTcN complex has been prepared by using SnCl2 as reductant. The effect of pH on RCP has been investigated. In the biodistribution study of 99mTcN-BMPBDA in mice
high myocardial uptake and rapid clearance from blood were demonstrated. After i.v. administration
24.53%ID·g-1 of 99mTcN-BMPBDA was extracted into heart at 2 minutes. However
the residence time of 99mTcN-BMPBDA in heart was not long
7.97%ID·g-1 of 99mTcN-BMPBDA retained in heart 30 minutes after injection. The activity clearance from blood is rapid and the clearance half-life is less than 15 minutes
but the activity level in blood is high. This study may be valuable for the design of new 99mTcN complex for myocardial perfusion imaging.
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