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Labeling bombesin-like peptide with 99mTc via hydrazinonicotinamide: description of optimized radiolabeling conditions

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Abstract

Bombesin (BNN)-like peptides have very high binding affinity for the gastrin-releasing peptide (GRP) receptor. The goal of the current study was to optimize the labeling conditions of a new 99mTc-radiolabeled BNN-like peptide based on the bifunctional chelating ligand HYNIC using different co-ligands (EDDA and tricine). The radiolabeling conditions (pH, amount of co-ligand, amount of stannous chloride, temperature and reaction time) for newly-formed 99mTc-tricine-HYNIC-Q-Litorin and 99mTc-EDDA-HYNIC-Q-Litorin were optimized and evaluated by RHPLC and RTLC. Radiochemical yields for 99mTc-tricine-HYNIC-Q-Litorin and 99mTc-EDDA-HYNIC-Q-Litorin were 98.0 ± 1.7 and 97.5 ± 2.5%, respectively. When EDDA was used as co-ligand, the labeling of 99mTc-EDDA-HYNIC-Q-Litorin was optimal in the following reaction mixture: HYNIC-peptide: EDDA: 10 μg/5 mg, pH 3, SnCl2 concentration: 12 μg/0.1 mL, reaction temperature: 100 °C, reaction time: 15 min. Besides, the optimum conditions were HYNIC-peptide:tricine: 10 μg/50 mg, pH 5, SnCl2 concentration: 12 μg/0.1 mL, reaction temperature: 100 °C, reaction time: 15 min for preparing 99mTc-tricine-HYNIC-Q-Litorin. The manufactured 99mTc-HYNIC-Q-Litorin conjugates may offer new possibilities for imaging cancer cells expressing bombesin receptors.

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Acknowledgements

The authors gratefully acknowledge the financial support received from the Scientific and Technological Research Council of Turkey, Scientific Project (TUBITAK Number 108S200).

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Authors and Affiliations

  1. Department of Nuclear Applications, Institute of Nuclear Science, Ege University, Bornova, 35100, Izmir, Turkey

    F. Yurt Lambrecht, K. Durkan & E. Bayrak

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  1. F. Yurt Lambrecht
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  2. K. Durkan
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  3. E. Bayrak
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Correspondence to F. Yurt Lambrecht.

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Yurt Lambrecht, F., Durkan, K. & Bayrak, E. Labeling bombesin-like peptide with 99mTc via hydrazinonicotinamide: description of optimized radiolabeling conditions. J Radioanal Nucl Chem 284, 539–545 (2010). https://doi.org/10.1007/s10967-010-0530-8

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  • DOI: https://doi.org/10.1007/s10967-010-0530-8

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