Synthesis of fluorine-18 radio-labeled serum albumins for PET blood pool imaging
| Autor: | M.V. Green, Olga Vasalatiy, Peter L. Choyke, Changhui Li, Mark C. Williams, Biying Xu, Gary L. Griffiths, Vince L. Coble, Elaine M. Jagoda, Falguni Basuli, Jurgen Seidel, Karen Wong |
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| Rok vydání: | 2015 |
| Předmět: |
Fluorine Radioisotopes
Cancer Research Biodistribution Serum albumin Niacin Article law.invention law medicine Animals Humans Distribution (pharmacology) Tissue Distribution Radiology Nuclear Medicine and imaging Incubation Serum Albumin Radiochemistry Chromatography medicine.diagnostic_test biology Chemistry Gated Blood-Pool Imaging Human serum albumin Rats Biochemistry Positron emission tomography Isotope Labeling Positron-Emission Tomography biology.protein Recombinant DNA Molecular Medicine medicine.drug |
| Zdroj: | Nuclear Medicine and Biology. 42:219-225 |
| ISSN: | 0969-8051 |
| DOI: | 10.1016/j.nucmedbio.2014.11.011 |
| Popis: | We sought to develop a practical, reproducible and clinically translatable method of radiolabeling serum albumins with fluorine-18 for use as a PET blood pool imaging agent in animals and man. Fluorine-18 radiolabeled fluoronicotinic acid-2,3,5,6-tetrafluorophenyl ester, [(18)F]F-Py-TFP was prepared first by the reaction of its quaternary ammonium triflate precursor with [(18)F]tetrabutylammonium fluoride ([(18)F]TBAF) according to a previously published method for peptides, with minor modifications. The incubation of [(18)F]F-Py-TFP with rat serum albumin (RSA) in phosphate buffer (pH9) for 15 min at 37-40 °C produced fluorine-18-radiolabeled RSA and the product was purified using a mini-PD MiniTrap G-25 column. The overall radiochemical yield of the reaction was 18-35% (n=30, uncorrected) in a 90-min synthesis. This procedure, repeated with human serum albumin (HSA), yielded similar results. Fluorine-18-radiolabeled RSA demonstrated prolonged blood retention (biological half-life of 4.8 hours) in healthy awake rats. The distribution of major organ radioactivity remained relatively unchanged during the 4 hour observation periods either by direct tissue counting or by dynamic PET whole-body imaging except for a gradual accumulation of labeled metabolic products in the bladder. This manual method for synthesizing radiolabeled serum albumins uses fluorine-18, a widely available PET radionuclide, and natural protein available in both pure and recombinant forms which could be scaled up for widespread clinical applications. These preclinical biodistribution and PET imaging results indicate that [(18)F]RSA is an effective blood pool imaging agent in rats and might, as [(18)F]HSA, prove similarly useful as a clinical imaging agent. |
| Databáze: | OpenAIRE |
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