~(99m)Tc标记“3 1”混合配体心血池显像剂的研究

合成了一种新的含有ＳＮＮ结构的三齿配体Ｎ＇－（２巯基－２－甲基异丙基）－Ｎ,Ｎ－二乙基乙二胺（ＭＤＥＤＡ）。用９９ｍＴｃ－葡庚糖配体交换法与不同的单齿硫酸制备了４种９９ｍＴｃ的“３＋１”混配配合物,标记率均大于９０％。对标记率的影响因素如ｐＨ、温度等作了探讨,并作了小鼠体内的分布实验和家兔的ＳＰＥＣＴ显像。实验表明这些配合物在血中的摄取和滞留远远超过了其他脏器,其中以配合物５ｃ的血滞留最好,有望达到血池显像剂的要求。

An investigation of ~(99m)Tc-labeled"3 1" mixed ligand complexes as potential blood-pool imaging agents

A new tridentate N-(2-mercapto-2-methylpropyl)- N,N-diethylethylene diamine (MDEDA) containing the SNN donor was synthesized and characterized by IR and 1H NMR. The tridentate and various monodentate thiols using 99mTc(V)-gluconate as precusor, chelates to the TcO3 core. Thus four "3 1," mixed ligand complexes of general formula TcO(Et2NCH2CH2 NCHC(CH3)2S] SR] were prepared. The labeling efficiency were all higher than 90%. The effects of pH value, temperature and reaction time were studied. The biodistribution results in mice and rabbits indicated that the uptake and retention of these complexes in blood was much higher and longer than those in other organs. The retention of complex 5c can be retend in blood was longer than the retention of others. Perhaps it can satisfy the requirement of blood-pool imaging agent.