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Development of a 68Ga-Fluorinated Porphyrin Complex as a Possible PET Imaging Agent

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Abstract

Aim

Due to the interesting pharmacologic properties of porphyrins, the idea of developing a possible tumor imaging agent using PET by incorporating 68Ga into a suitable porphyrin ligand was investigated.

Methods

68Ga-labeled 5,10,15,20-tetrakis(pentafluoro-13 phenyl) porphyrin (68Ga-TFPP) was prepared using freshly eluted [68Ga]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.

Results

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.

Conclusion

The radiolabeled porphyrin complex demonstrated potential for further imaging studies in other tumor models.

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Acknowledgments

Authors wish to thank Mr. S. Daneshvari for conducting the animal studies.

Conflicts of Interest

The authors declare no conflict of interest.

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Authors and Affiliations

  1. 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

    Yousef Fazaeli, Khosro Ardaneh, Ali Rahiminejad, Fatemeh Bolourinovin, Sedigheh Moradkhani & Abbas Majdabadi

  2. Radiopharmaceutical Research and Development Lab, Nuclear Science and Technology Research Institute (NSTRI), P.O. Box:14395-836, Tehran, Iran

    Amir R. Jalilian

  3. Department of Chemistry, Shahid Beheshti University, G.C., P.O. Box 19396–4716, Tehran, Iran

    Mostafa M. Amini

Authors
  1. Yousef Fazaeli
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  2. Amir R. Jalilian
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  3. Mostafa M. Amini
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  4. Khosro Ardaneh
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  5. Ali Rahiminejad
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  6. Fatemeh Bolourinovin
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  7. Sedigheh Moradkhani
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  8. Abbas Majdabadi
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Correspondence to Amir R. Jalilian.

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Fazaeli, Y., Jalilian, A.R., Amini, M.M. et al. Development of a 68Ga-Fluorinated Porphyrin Complex as a Possible PET Imaging Agent. Nucl Med Mol Imaging 46, 20–26 (2012). https://doi.org/10.1007/s13139-011-0109-5

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  • DOI: https://doi.org/10.1007/s13139-011-0109-5

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