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Preparation and evaluation of a new 99mTc labeled bombesin derivative for tumor imaging

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Abstract

A variety of human tumors like prostate and breast cancer express bombesin receptors. Due to this a new bombesin analogue was labeled with 99mTc via HYNIC and tricine as a coligand and investigated further. Peptide was synthesized on a solid phase using 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 human serum at 37 °C up to 24 h. Internalization was studied with the human GRP receptor cell line PC-3. The biodistribution was studied in mice. Labeling yield of >98% was obtained corresponding to a specific activity of ~80.9 GBq/μmol. Radiopeptide internalization into PC-3 cells was moderate and specific (10.7 ± 1.2% at 4 h). A high and specific GRP receptor expressing mouse tumor and pancreas uptake (1.12 ± 0.08 and 1.04 ± 0.11% ID/g after 1 h respectively) was also determined.

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Acknowledgement

The authors wish to thank Mr. Mirfallah, Mr. Mazidi 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. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran

    N. Sadeghzadeh, S. E. Sadat Ebrahimi & A. Shafiee

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

    M. Gandomkar, R. Najafi & M. Shafiei

  3. Endocardiology and Metabolism Research Center, Tehran University of Medical Sciences, Tehran, Iran

    B. Larijani

Authors
  1. N. Sadeghzadeh
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  2. M. Gandomkar
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  3. R. Najafi
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  4. M. Shafiei
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  5. S. E. Sadat Ebrahimi
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  6. A. Shafiee
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  7. B. Larijani
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Corresponding author

Correspondence to S. E. Sadat Ebrahimi.

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Sadeghzadeh, N., Gandomkar, M., Najafi, R. et al. Preparation and evaluation of a new 99mTc labeled bombesin derivative for tumor imaging. J Radioanal Nucl Chem 283, 181–187 (2010). https://doi.org/10.1007/s10967-009-0138-z

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  • DOI: https://doi.org/10.1007/s10967-009-0138-z

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