Mach R H, Kung H F, Guo Y Z, Yu C C, Subramanyam V, Calabrese J C
Department of Radiology, Hospital of the University of Pennsylvania, Philadelphia 19104.
Int J Rad Appl Instrum B. 1989;16(8):829-37. doi: 10.1016/0883-2897(89)90168-2.
Two new ligand systems for complexation with 99mTc were prepared. The two analogs of bisaminoethanethiol (BAT): N,N'-bis(2-methyl-2-mercaptopropyl)-2,2-dimethylpropylenediamin e (PAT-HM) and N,N'-bis[2-(2-ethyl-1-mercaptopropyl)] ethylenediamine (TMR), form neutral and lipid soluble complexes with 99mTc that readily penetrate the blood-brain barrier following i.v. injection into rats. Although the 99mTc chelates do not display the prolonged brain retention required for use in single photon emission computed tomographic imaging studies, the fact that each ligand forms a neutral and lipid-soluble complex of high chemical stability when coordinated with 99mTc warrants further investigation to increase the site- and organ-specificity of these agents.
制备了两种用于与99mTc络合的新配体系统。双氨基乙硫醇（BAT）的两种类似物：N，N'-双（2-甲基-2-巯基丙基）-2，2-二甲基丙二胺（PAT-HM）和N，N'-双[2-（2-乙基-1-巯基丙基）]乙二胺（TMR），与99mTc形成中性且脂溶性的络合物，静脉注射到大鼠体内后可轻易穿透血脑屏障。尽管99mTc螯合物不显示单光子发射计算机断层成像研究中所需的长时间脑内滞留，但每个配体与99mTc配位时形成具有高化学稳定性的中性且脂溶性络合物这一事实，值得进一步研究以提高这些试剂的位点和器官特异性。
