Labeling bombesin-like peptide with 99mTc via hydrazinonicotinamide: description of optimized radiolabeling conditions
| Autor: | Kubra Durkan, F. Yurt Lambrecht, Elif Bayrak |
|---|---|
| Rok vydání: | 2010 |
| Předmět: |
chemistry.chemical_classification
Tricine Chromatography Health Toxicology and Mutagenesis Public Health Environmental and Occupational Health Bombesin Peptide Pollution Combinatorial chemistry Analytical Chemistry chemistry.chemical_compound Nuclear Energy and Engineering chemistry Gastrin-releasing peptide Bombesin-like peptides Radiology Nuclear Medicine and imaging Chelation Bifunctional Spectroscopy Conjugate |
| Zdroj: | Journal of Radioanalytical and Nuclear Chemistry. 284:539-545 |
| ISSN: | 1588-2780 0236-5731 |
| DOI: | 10.1007/s10967-010-0530-8 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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