Radiosynthesis of a novel potential adenosine A3 receptor ligand, 5-ethyl 2,4-diethyl-3-((2-[18F]fluoroethyl)sulfanylcarbonyl)-6-phenylpyridine-5-carboxylate ([18F]FE@SUPPY:2)
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Daniela Haeusler
Abstract
Since, to date very limited information on the distribution and function of the adenosine A3 receptor is available, the development of suitable radioligands is needed. Recently, we introduced [ 18F]FE@SUPPY (5-(2-[ 18F]fluoroethyl) 2,4-diethyl-3-(ethylsulfanylcarbonyl)-6-phenylpyridine-5-carboxylate) as the first PET-ligand for the A3R. Regarding the metabolic profile – this class of dialkylpyridines comprises two ester functions within one molecule, one carboxylic and one thiocarboxylic – one could expect carboxylesterases significantly contributing to cleavage and degradation. Therefore, our aim was the development of [ 18F]FE@SUPPY:2 (5-ethyl 2,4-diethyl-3-((2-[ 18F]fluoroethyl)sulfanylcarbonyl)-6-phenylpyridine-5-carboxylate), the functional isomer containing the label at the thiocarboxylic moiety.
For satisfactory yields in high scale radiosyntheses, a reaction temperature of 75 °C has to be applied for at least 20 min using 20 mg/mL of precursor. So far, 6 complete high-scale radiosyntheses were performed. Starting from an average of 51.2±21.8 GBq (mean±SD) [ 18F]fluoride, 5.8±4.1 GBq of formulated [ 18F]FE@SUPPY:2 (12.0±5.4%, based on [ 18F]fluoride, not corrected for decay) were prepared in 75±8 min.
© by Oldenbourg Wissenschaftsverlag, München, Germany
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Artikel in diesem Heft
- Production and separation of no-carrier-added 93,94,95Tc from 9Be activated yttrium target
- Charged particle induced reaction cross section data for production of the emerging medically important positron emitter 64Cu: A comprehensive evaluation
- Determination of 126Sn half-life from ICP-MS and gamma spectrometry measurements
- Investigation of K to L shell/subshell vacancy transitions of Zn and Fe in FexZn1-x thin film alloys
- X-ray absorption spectroscopic study of trivalent and tetravalent actinides in solution at varying pH values
- Kinetic and thermodynamic studies on the adsorption of U(VI) ions on densely crosslinked poly(methacrylic acid) from aqueous solutions
- Extraction of americium(III) from nitric acid medium by CMPO-TBP extractants in ionic liquid diluent
- Uranium, plutonium and neptunium co-recovery with high nitric acid concentration in extraction section by simplified solvent extraction process
- Separation of 109Cd from silver targets by nanohematite
- An adapted purification procedure to improve the quality of 90Y for clinical use
- Novel polymer vectors of 64Cu
- Radiosynthesis of a novel potential adenosine A3 receptor ligand, 5-ethyl 2,4-diethyl-3-((2-[18F]fluoroethyl)sulfanylcarbonyl)-6-phenylpyridine-5-carboxylate ([18F]FE@SUPPY:2)
- Determination of solubility parameters of cobalt(II) and indium(III) oxinates by tracer technique
- Evaluation of trace elements in chewing tobacco and snuff using instrumental neutron activation analysis (INAA) and atomic absorption spectroscopy (AAS)
