本研究的目的是评估用于脑肿瘤靶向的放射性金属络合物平台。在此，我们介绍了一种新的卟啉衍生物，5,10,15,20-(四-N,N-二甲基-4-氨基苯基)卟啉(TDAP)，其中四个N,N-二甲基-4-对苯二胺( DMPD）部分与放射性金属 64Cu 标记的卟啉缀合。相对于未修饰的卟啉，DMPD 在体内保留时间和肿瘤靶向能力方面影响卟啉的药代动力学。 [64Cu]Cu-TDAP 在 U87MG 胶质母细胞瘤细胞中表现出比 [64Cu]Cu-卟啉更强的增强作用，特别是在细胞质和细胞核中，表明其肿瘤靶向特性和作为治疗剂的潜在用途。在荷有脑肿瘤的小鼠的皮下和原位模型中，通过正电子发射断层扫描成像，[64Cu]Cu-TDAP 在肿瘤部位清晰可见，并且肿瘤与脑的比率高达 13。 [64Cu]Cu -TDAP作为一种适合脑肿瘤早期诊断和治疗的新型诊断剂值得关注。

The aim of this study is to evaluate a radioactive metal complex platform for brain tumor targeting. Herein, we introduce a new porphyrin derivative, 5,10,15,20-(tetra-N,N-dimethyl-4-aminophenyl)porphyrin (TDAP), in which four N,N-dimethyl-4-p-phenylenediamine (DMPD) moieties are conjugated to the porphyrin labeled with the radiometal 64Cu. DMPD affected the pharmacokinetics of porphyrin in terms of retention time in vivo and tumor-targeting ability relative to those of unmodified porphyrin. [64Cu]Cu-TDAP showed stronger enhancement than [64Cu]Cu-porphyrin in U87MG glioblastoma cells, especially in the cytoplasm and nucleus, indicating its tumor-targeting properties and potential use as a therapeutic agent. In the subcutaneous and orthotopic models of brain-tumor-bearing mice, [64Cu]Cu-TDAP was clearly visualized in the tumor site via positron emission tomography imaging and showed a tumor-to-brain ratio as high as 13. [64Cu]Cu-TDAP deserves attention as a new diagnostic agent that is suitable for the early diagnosis and treatment of brain tumors.