A 2A Adenosine Receptor Agonists With Last‐Step Enzymatic 18 F‐Labelling Potential (Fluorinase) for Positron Emission Tomography (PET)

This is the authors' abstract. We don't add key points for this paper.

New agonists of the A 2A receptor are reported with 18 F‐labelling potential for positron emission tomography (PET). These were designed by exploiting common binding interactions of substrates for the fluorinase and agonists of the human A 2A adenosine receptor. Target compounds were structurally inspired by the selective A 2A receptor agonist CGS21680 . The new agonists were synthesised and their affinities for the human A 2A receptor evaluated through radioligand displacement assays. 18 F‐Labelled analogues of the new agonists for potential PET radiotracer applications are now accessible through last‐step radiosynthesis using the fluorinase enzyme and [ 18 F]fluoride.