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Radiosynthesis and Biological Evaluation of [^(111)In]-5, 10, 15, 20-Tetrakis (Pentafluorophenyl) Porphyrin Complex as a Possible Imaging Agent

並列摘要


Porphyrins are interesting derivatives with low toxicity, tumor avidity, and rapid wash-out suggested as potential radiopharmaceuticals in radiolabeled form. In this work, [^(111)In] labeled 5, 10, 15, 20-tetrakis (pentafluorophenyl) porphyrin ([^(111)In]-TFPP) was prepared using freshly prepared [^(111)In]InCl3 and 5,10,15,20-tetrakis (pentafluorophenyl) porphyrin (H_2TFPP) for 60 min at 100C (radiochemical purity: >99% ITLC, >99% HPLC, specific activity: 13-14 GBq/mmol). Stability of the complex was checked in final formulation and human serum for 48 h. The partition coefficient was calculated for the compound (log P=0.69). The biodistribution of the labeled compound in vital organs of wild-type rats and fibrosarcoma-bearing mice was studied using scarification studies and SPECT up to 24 h. A detailed comparative pharmacokinetic study performed for 111In cation and [^(111)In]-TFPP performed up to 24h. The complex is mostly washed out from the circulation through kidneys and liver. The tumor:blood and tumor: muscle ratios 24 h post injection were 1.44 and 66 respectively.

並列關鍵字

Porphyrins In-111 Fibrosarcoma Biodistribution SPECT

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