1207955-08-5Relevant academic research and scientific papers
One step radiosynthesis of 6-[18F]fluoronicotinic acid 2,3,5,6-tetrafluorophenyl ester ([18F]F-Py-TFP): A new prosthetic group for efficient labeling of biomolecules with fluorine-18
Olberg, Dag E.,Arukwe, Joseph M.,Grace, David,Hjelstuen, Ole K.,Solbakken, Magne,Kindberg, Grete M.,Cuthbertson, Alan
experimental part, p. 1732 - 1740 (2010/07/16)
The labeling of biomolecules for positron emission tomography (PET) with no-carrier-added fluorine-18 is almost exclusively accomplished using prosthetic groups in a two step procedure. The inherent complexity of the process renders full automation a challenge and leads to protracted synthesis times. Here we describe a new 18F-labeled prosthetic group based on, nicotinic acid tetrafiuorophenyl ester. Reaction of [18F]fluoride at 40°C with the trimethylammonium precursor afforded 6-[18F]fluoronicotinic acid tetrafiuorophenyl ester ([18F]F-Py-TFP) directly in 60-70% yield. [18F]F-Py-TFP was conveniently purified by Sep-Pak cartridge prior to incubation with a peptide containing the RGD sequence. The desired conjugate was formed rapidly and in good yields. An in vitro receptor-binding assay for the integrin αvβ3 was established to explore competition with peptide and peptidomlmetic prepared from F-Py-TFP with 125I-echlstatin. The nonradioactive conjugates were found to possess high binding affinities with calculated Ki values in the low nanomolar range.
RADIOLABELLING REAGENTS AND METHODS
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Page/Page column 9-10, (2010/11/03)
The present invention relates to reagents and methods for [18F]-fluorination of biomolecules, particularly of peptides. The resultant 18F-labelled compounds are useful as radiopharmaceuticals, specifically for use in Positron Emission Tomography (PET).
