Papadopoulos M, Chiotellis E, Varvarigou A, Mastrostamatis S, Cotsyfakis C, Vavouraki H, Stathaki S
Radiopharmaceuticals Laboratory, Institute of Radioisotopes and Radiodiagnostics, NCSR Demokritos, Attiki, Greece.
Nucl Med Biol. 1993 Jan;20(1):101-4. doi: 10.1016/0969-8051(93)90142-h.
A series of 99mTc-DADT complexes substituted with heterocyclic amines were synthesized and tested for their ability to cross the BBB. Each 99mTc-DADT complex analysed by HPLC was found to consist of two epimers. The more lipophilic epimers were biodistributed in mice. The data demonstrated a significant brain uptake (3-12% dose/g whole brain) and a high lung accumulation (11-85% dose/g) at 2 min p.i. Between the partition coefficients of the technetium complexes, a linear correlation for lung accumulation was observed, while a parabolic curve for brain uptake was found.
合成了一系列用杂环胺取代的99mTc-DADT配合物，并测试了它们穿越血脑屏障的能力。通过高效液相色谱分析的每种99mTc-DADT配合物均由两个差向异构体组成。亲脂性更强的差向异构体在小鼠体内的生物分布情况。数据显示，注射后2分钟时，脑摄取量显著（3-12%剂量/克全脑），肺蓄积量高（11-85%剂量/克）。在锝配合物的分配系数之间，观察到肺蓄积呈线性相关，而脑摄取呈抛物线曲线。
