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Synthesis and evaluation of a new bombesin analog labeled with 99mTc as a GRP receptor imaging agent

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Abstract

Tumors such as prostate, small cell lung cancer, breast, gastric and colon cancer are known to overexpress receptors to bombesin (BBN). In this study, a new bombesin analogue was labeled with 99mTc via HYNIC and tricine/EDDA as coligands and investigated further. HYNIC-GABA-Bombesin (7–14) NH2 was synthesized using a standard Fmoc strategy. Labeling with 99mTc was performed at 100 °C for 10 min and radiochemical analysis involved ITLC and HPLC methods. The stability of radiopeptide was checked in the presence of humane serum at 37 °C up to 24 h. The receptor bound internalization and externalization rates were studied in GRP receptor expressing PC-3 cells. Biodistribution of radiopeptide was studied in nude mice bearing PC-3 tumor. Labeling yield of >98% was obtained corresponding to a specific activity of ~2.6 MBq/nmol. Peptide conjugate showed good stability in the presence of human serum. The radioligand showed high and specific internalization into PC-3 cells (14.63 ± 0.41% at 4 h). In biodistribution studies, a receptor-specific uptake was observed in GRP-receptor-positive organs so that after 4 h the uptakes in mouse tumor and pancreas were 1.31 ± 0.18 and 1.2 ± 0.13% ID/g, respectively.

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Acknowledgments

The authors wish to thank Mr. Mirfallah and Mr. Talebi of the radioisotope department (AEOI) for providing sodium pertechnetate and assistance in quality control tests.

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Authors and Affiliations

  1. Nuclear Science Research School, Nuclear Science and Technology Research Institute (NSTRI), Atomic Energy Organization of Iran, Tehran, Iran

    S. P. Shirmardi, M. Gandomkar, M. Mazidi, M. Shafiei & M. Ghannadi Maragheh

  2. Faculty of Nuclear Engineering and Physics, Amirkabir University of Technology, Tehran, Iran

    S. P. Shirmardi

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  1. S. P. Shirmardi
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  2. M. Gandomkar
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Correspondence to M. Gandomkar.

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Shirmardi, S.P., Gandomkar, M., Mazidi, M. et al. Synthesis and evaluation of a new bombesin analog labeled with 99mTc as a GRP receptor imaging agent. J Radioanal Nucl Chem 288, 327–335 (2011). https://doi.org/10.1007/s10967-011-0985-2

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  • DOI: https://doi.org/10.1007/s10967-011-0985-2

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