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Preparation and evaluation of a new neurotensin analog labeled with 99mTc for targeted imaging of neurotensin receptor positive tumors

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Abstract

Neurotensin receptors are overexpressed in several human tumors and can be targets for tumors diagnosis and therapy. In this study, a new neurotensin analogue was labeled with 99mTc via HYNIC and tricine/EDDA as coligands and investigated further. [HYNIC0, Gly7, Lys9, d-Tyr11]-Neurotensin (7–13) 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 neurotensin receptor expressing HT-29 cells. Biodistribution of radiopeptide was studied in nude mice bearing HT-29 tumor. Labeling yield of 98.6 ± 0.54 % (n = 3) was obtained corresponding to a specific activity of 81 MBq/nmol. Peptide conjugate showed good stability in the presence of human serum. The radioligand showed specific internalization into HT-29 cells (12.43 ± 0.52 % at 4 h). In biodistribution studies, a receptor-specific uptake was observed in neurotensin receptor positive organs so that after 1 h the uptakes in mouse intestine and tumor were 0.87 ± 0.16 and 0.63 ± 0.12 % 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. Department of Biology, Science and Research Branch, Islamic Azad University, P.O. Box 14515-775, Tehran, Iran

    Nakisa Zarrabi Ahrabi & Kazem Parivar

  2. Nuclear Science Research School, Nuclear Science and Technology Research Institute (NSTRI), Atomic Energy Organization of Iran (AEOI), End of Karegar Ave., P.O. Box 11365-3486, Tehran, Iran

    Mostafa Erfani & Amir Reza Jalilian

  3. Research Institute for Nuclear Medicine, Tehran University of Medical Sciences, Tehran, Iran

    Davood Beiki

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  1. Nakisa Zarrabi Ahrabi
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  2. Mostafa Erfani
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  3. Kazem Parivar
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  5. Amir Reza Jalilian
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Correspondence to Nakisa Zarrabi Ahrabi.

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Ahrabi, N.Z., Erfani, M., Parivar, K. et al. Preparation and evaluation of a new neurotensin analog labeled with 99mTc for targeted imaging of neurotensin receptor positive tumors. J Radioanal Nucl Chem 299, 461–469 (2014). https://doi.org/10.1007/s10967-013-2795-1

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  • DOI: https://doi.org/10.1007/s10967-013-2795-1

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