A <sub>2A</sub> Adenosine Receptor Agonists With Last‐Step Enzymatic <sup>18</sup> F‐Labelling Potential (Fluorinase) for Positron Emission Tomography (PET)
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.
Authors
- Laura H. Heitman (ORCID: https://orcid.org/0000-0002-1381-8464)
- Phillip T. Lowe (ORCID: https://orcid.org/0000-0003-1568-0750)
- Sergio Dall’Angelo (ORCID: https://orcid.org/0000-0001-9377-0474)
- Nicolas Charalambous
- Rongfang Liu
- David O’Hagan
- Carina Schleidt
Institutions
- University of St Andrews (GB)
- University of Aberdeen (GB)
- NHS Grampian (GB)
- Centre for Human Drug Research (NL)
Publication Details
- Journal
- European Journal of Organic Chemistry
- Published
- 2025-12-26
- DOI
- https://doi.org/10.1002/ejoc.202501125
- Primary Topic
- Medical Imaging Techniques and Applications
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- Engineering and Physical Sciences Research Council