Papadopoulos M, Stathaki S, Mastrostamatis S, Varvarigou A, Chiotellis E
Radiopharmaceuticals Laboratory, Institute of Radiosotopes and Radiodiagnostics, NCSR Demokritos, Attiki, Greece.
Nucl Med Biol. 1993 Jan;20(1):105-15. doi: 10.1016/0969-8051(93)90143-i.
Alkylpiperidinyl and alkylpyrrolidinyl 99mTc-DADT complexes were synthesized and tested for their ability to cross the BBB. Each complex was a mixture of two epimers separated by HPLC. More lipophilic epimers were biologically evaluated in mice, at various time intervals. Similar biodistribution patterns were obtained for both piperidinyl and pyrrolidinyl DADT-complexes. Brain uptake or retention was influenced by the heterocyclic amine introduced into the DADT backbone. Subcellular concentration of selected 99mTc-DADT complexes was more profound in crude nuclear and post-microsomal fractions. Moreover, interaction of 99mTc-2,2,6,6,9,9-hexamethyl-4,7-diaza-4-(3-methylpyrroli dinyl)-ethyl-1,10- decanedithiol with either lipids or microsomes of whole brain was almost unaffected by time. This may suggest that a possible selective site of interaction and metabolism for DADT complexes occurs in brain.
合成了烷基哌啶基和烷基吡咯烷基99mTc - DADT配合物，并测试了它们穿过血脑屏障的能力。每个配合物都是通过高效液相色谱分离的两种差向异构体的混合物。在不同时间间隔对小鼠体内更具亲脂性的差向异构体进行了生物学评估。哌啶基和吡咯烷基DADT配合物获得了相似的生物分布模式。脑摄取或滞留受引入DADT主链的杂环胺影响。所选99mTc - DADT配合物在粗核和微粒体后级分中的亚细胞浓度更高。此外，99mTc - 2,2,6,6,9,9 - 六甲基 - 4,7 - 二氮杂 - 4 - (3 - 甲基吡咯烷基) - 乙基 - 1,10 - 癸二硫醇与全脑脂质或微粒体的相互作用几乎不受时间影响。这可能表明DADT配合物在脑中存在可能的选择性相互作用和代谢位点。
