Abstract
Introduction: Since the Adenosine-A3-receptor was identified in the late 1990´s, there is little data available de- scribing its distribution in vivo. Recently, we introduced ( 18 F)FE@SUPPY as the first PET-tracer for this receptor. In the present investigation we translated this fluoroethyl-ester into the fluoroethyl-thioester ( 18 F)FE@SUPPY:2 (5-ethyl 2,4- diethyl-3-((2-( 18 F)fluoroethyl) sulfanylcarbonyl)-6-phenylpyridine-5-carboxylate). Aims of the present study were the evaluation of (1) the automatized preparation of both ( 18 F)FE@SUPPY-derivatives, (2) the biodistribution of ( 18 F)FE@SUPPY:2, (3) the lipophilicity and (4) the comparison of the findings of ( 18 F)FE@SUPPY and ( 18 F)FE@SUPPY:2. Methods: The automated preparations of both ( 18 F)FE@SUPPY-analogs were performed on a GE TRACERlab FxFN syn- thesizer using suitable precursors. Biodistribution experiments were performed using Sprague-Dawley rats/Him:OFA. Lipophilicity of the compounds was determined using an HPLC assay. Results: 22 automated radiosyntheses were performed for both radiotracers. Specific radioactivity was 70 ± 26GBq/� mol for ( 18 F)FE@SUPPY and 340 ± 140GBq/� mol for ( 18 F)FE@SUPPY:2. Biodistribution experiments evinced bowels and liver as organs with highest uptake and intermediate uptake in kidney, lung and heart. LogP values of both molecules ranged from 3.99 to 4.12 at different pH. Conclusion: From a radiopharmaceutical perspective, drastically better specific radioactivities would militate in favour of ( 18 F)FE@SUPPY:2; preclinical evaluations, so far, do not permit the decision upon the selection of the optimum ( 18 F)FE@SUPPY-derivative. With ( 18 F)FE@SUPPY:2, we are able to provide a second potential tracer that could help to further characterize the still quite unexplored Adenosine-A3-receptor.
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