Chiotellis E, Varvarigou A D, Maina T, Stassinopoulou C I
Radiodiagnostic Products Department, National Research Center of Physical Sciences Demokritos, Aghia Paraskevi Attikis, Greece.
Int J Rad Appl Instrum B. 1988;15(2):215-23. doi: 10.1016/0883-2897(88)90091-8.
Several new 99mTc aminodithiols were prepared and evaluated comparatively in experimental animals. The ligands were diamine, triamine or tetramine dithiols. Substituents were either attached on one of the nitrogens or introduced in between the two nitrogens of diamino dithiol (DADT) backbone. 99mTc-derivatives prepared by coupling DADT to secondary amines via ethylene group showed in mice high initial brain uptake and significant retention in brain tissue. These preparations were mixtures of more than one 99mTc-complex differing in brain uptake and clearance from the brain. The highest brain retention (brain to blood ratio 2.53, 15 min p.i.) was achieved with the 99mTc-complex prepared by coupling DADT with ethylene pyrrolidine. Lengthening the chain between the nitrogens of DADT moiety by introducing methyl or amino alkyl groups resulted in 99mTc-complexes with poor brain accumulation.
制备了几种新的99mTc氨基二硫醇，并在实验动物中进行了比较评估。这些配体为二胺、三胺或四胺二硫醇。取代基要么连接在其中一个氮原子上，要么引入二氨基二硫醇（DADT）主链的两个氮原子之间。通过乙烯基将DADT与仲胺偶联制备的99mTc衍生物在小鼠中显示出高初始脑摄取和在脑组织中的显著滞留。这些制剂是多种99mTc络合物的混合物，它们在脑摄取和从脑中清除方面存在差异。通过将DADT与乙烯基吡咯烷偶联制备的99mTc络合物实现了最高的脑滞留（注射后15分钟时脑血比为2.53）。通过引入甲基或氨基烷基延长DADT部分氮原子之间的链，得到的99mTc络合物脑蓄积性较差。
