心肌显像剂^(99m)TcN-BMPBDA的制备及动物体内分布研究

Preparaion and prelminary biodistribution in mice of ^(99m)TcN-BMPBDA for myocardial perfusion imaging

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.