一种新的N_2S_2配位体合成和~(99)Tc~mO标记及其生物分布研究

SYNTHESIS OF A NEW N_2S_2 LIGAND AND ITS LABELLING AND BIODISTRIBUTION OF ~(99)Tc~mO-BMPBDA IN MICE

摘要: 为了寻找新的具有灌注显像能力的99TcmO药物 ,合成了N2 S2 配位体———N ,N′ 二 ( 2 巯基丙基 ) 1 ,2 苯二胺 (BMPBDA)。以SnCl2 为还原剂 ,制备了放化纯大于 95 %的99TcmO BMPBDA。探讨了 pH值对99TcmO BMPBDA放化纯的影响 ,并对其在小鼠体内的生物分布进行了研究。结果表明 ,99TcmO BMPBDA在心肌中具有相当的初始摄取和较好的滞留。静脉注射后 2、30min时的心肌摄取率分别为 1 2 4、1 0 76 % /g。血清除较快 ,血半清除期小于 1 5min ,但血液中活度仍较高。本工作对设计新的99TcmO灌注显像药物具有参考价值。

Abstract: In order to find new 99 Tc mO complexes for perfusion imaging, a new N 2S 2 ligand of N, N' bis(2 mercaptopropyl) 1,2 benzenediamine(BMPBDA)has been synthesized and its 99 Tc mO complex has been prepared by using SnCl 2 as reductant. Effect of pH has been investigated. In the biodistribution study of 99 Tc mO BMPBDA in mice, high myocardial uptake and retention are demonstrated. After administration, 12.37 %/g of 99 Tc mO BMPBDA is extracted into heart in 2 min. The residence time of 99 Tc mO BMPBDA in heart is long, 10.76 %/g of 99 Tc m O BMPBDA retains in heart far 30 min postinjection. The activity clearance from blood is rapid and the clearance half life is less than 15 min, but the activity level in blood is high. This study may be valuable to the design of new 99 Tc mO complex for perfusion imaging.