Fazaeli Yousef, Jalilian Amir R, Amini Mostafa M, Ardaneh Khosro, Rahiminejad Ali, Bolourinovin Fatemeh, Moradkhani Sedigheh, Majdabadi Abbas
Nuclear Medicine Research Group, Agricultural, Medical and Industrial Research School (AMIRS), Nuclear Science and Technology Research Institute (NSTRI), P.O.Box: 31485-498, Karaj, Iran.
Radiopharmaceutical Research and Development Lab, Nuclear Science and Technology Research Institute (NSTRI), P.O. Box:14395-836, Tehran, Iran.
Nucl Med Mol Imaging. 2012 Mar;46(1):20-6. doi: 10.1007/s13139-011-0109-5. Epub 2011 Dec 16.
Due to the interesting pharmacologic properties of porphyrins, the idea of developing a possible tumor imaging agent using PET by incorporating (68)Ga into a suitable porphyrin ligand was investigated.
(68)Ga-labeled 5,10,15,20-tetrakis(pentafluoro-13 phenyl) porphyrin ((68)Ga-TFPP) was prepared using freshly eluted [(68)Ga]GaCl3 obtained from a 68Ge/68Ga generator developed in-house and 5,10,15,20-tetrakis(pentafluorophenyl)porphyrin (H2TFPP) for 60 min at 100°C.
The complex was prepared with high radiochemical purity (>99% ITLC, >99% HPLC, specific activity: 13-14 GBq/mmol). Stability of the complex was checked in the final formulation and in human serum for 5 h. The partition coefficient was calculated for the compound (log P = 0.62). The biodistribution of the labeled compound in vital organs of Swiss mice bearing fibrosarcoma tumors was studied using scarification studies and SPECT imaging up to 1 h. The complex was mostly washed out from the circulation through kidneys and liver. The tumor-to-muscle ratio 1 h post injection was 5.13.
The radiolabeled porphyrin complex demonstrated potential for further imaging studies in other tumor models.
由于卟啉具有有趣的药理学特性，因此研究了通过将（68）镓掺入合适的卟啉配体中开发一种可能用于正电子发射断层扫描（PET）的肿瘤显像剂的想法。
使用从内部开发的68锗/68镓发生器获得的新鲜洗脱的[（68）镓]氯化镓和5,10,15,20-四（五氟-13苯基）卟啉（H2TFPP）在100°C下制备60分钟，制备（68）镓标记的5,10,15,20-四（五氟苯基）卟啉（（68）镓-TFPP）。
该配合物以高放射化学纯度制备（>99% 薄层层析，>99% 高效液相色谱，比活度：13-14 GBq/mmol）。在最终制剂和人血清中检查该配合物5小时的稳定性。计算该化合物的分配系数（log P = 0.62）。使用划痕研究和单光子发射计算机断层扫描（SPECT）成像研究标记化合物在患有纤维肉瘤肿瘤的瑞士小鼠重要器官中的生物分布，长达1小时。该配合物大多通过肾脏和肝脏从循环中清除。注射后1小时肿瘤与肌肉的比值为5.13。
放射性标记的卟啉配合物在其他肿瘤模型中显示出进一步成像研究的潜力。
