A1 Refereed original research article in a scientific journal
19F/18F exchange synthesis for a novel [18F]S1P3-radiopharmaceutical
Authors: Johanna Rokka, Cesare Federico, Jori Jurttila, Anniina Snellman, Merja Haaparanta, Juha O Rinne, Olof Solin
Publisher: WILEY-BLACKWELL
Publication year: 2013
Journal: Journal of Labelled Compounds and Radiopharmaceuticals
Journal name in source: JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
Journal acronym: J LABELLED COMPD RAD
Number in series: 8
Volume: 56
Issue: 8
First page : 385
Last page: 391
Number of pages: 7
ISSN: 0362-4803
DOI: https://doi.org/10.1002/jlcr.3055
Abstract
F-19/F-18 isotope exchange is a useful method to label drug molecules containing F-19-fluorine with F-18 without modifying the drug molecule itself. Sphingosine-1-phosphate (S1P) is an important cellular mediator that functions by signaling through cell surface receptors. S1P is involved in several cell responses and may be related to many central nervous system disorders, including neural malfunction in Alzheimer's disease. In this study, [F-18]1-benzyl-N-(3,4-difluorobenzyl)-2-isopropyl-6-(2-methoxyethoxy)-1H-indole-3-carboxamide, a novel F-18-labeled positron emission tomography tracer for the S1P(3) receptor, was successfully synthesized using the F-19/F-18 isotope exchange reaction. Parameters of the reaction kinetics were studied, and correlations between the initial F-18-activity, the amount of precursor, radiochemical yield and specific activity (SA) were determined. Contrary to expectations, high initial F-18-activity decreased the radiochemical yield, and only a minor increase of SA occurred. F-19/F-18 exchange reaction is the use of 2 mu mol precursor with 20GBq of F-18-activity. F-18-activity and F-19/F-18 isotope exchange is used.
F-19/F-18 isotope exchange is a useful method to label drug molecules containing F-19-fluorine with F-18 without modifying the drug molecule itself. Sphingosine-1-phosphate (S1P) is an important cellular mediator that functions by signaling through cell surface receptors. S1P is involved in several cell responses and may be related to many central nervous system disorders, including neural malfunction in Alzheimer's disease. In this study, [F-18]1-benzyl-N-(3,4-difluorobenzyl)-2-isopropyl-6-(2-methoxyethoxy)-1H-indole-3-carboxamide, a novel F-18-labeled positron emission tomography tracer for the S1P(3) receptor, was successfully synthesized using the F-19/F-18 isotope exchange reaction. Parameters of the reaction kinetics were studied, and correlations between the initial F-18-activity, the amount of precursor, radiochemical yield and specific activity (SA) were determined. Contrary to expectations, high initial F-18-activity decreased the radiochemical yield, and only a minor increase of SA occurred. F-19/F-18 exchange reaction is the use of 2 mu mol precursor with 20GBq of F-18-activity. F-18-activity and F-19/F-18 isotope exchange is used.
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