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PET imaging of A2A adenosine receptors

Preclinical evaluation of a 18F-labelled A2A adenosine receptor ligand for in vivo brain imaging

Cerebral A2A adenosine receptors (A2AAR) play an important role in the regulation of locomotion, sleep-wake rhythm, anxiety, memory function and perception. Due to this regulatory function, the A2AAR is associated with the pathogenesis of various diseases such as Parkinson's disease, Huntington's disease, depression, and substance dependence. The examination of this receptor with positron emission tomography (PET) in the healthy and diseased brain may therefore provide fundamental insights into brain function and the development of neurological diseases. A2AAR-PET has therefore potentials to become a promising tool for the diagnosis of these diseases.

In cooperation with the Institute of Nuclear Chemistry (INM-5) we aim to establish a selective PET radioligand for the A2AAR that allows its visualization and quantification in the brain. We are investigating various 18F-labelled compounds regarding their binding capacities in rat and human brain specimens (in vitro studies) as well as in PET investigations in rats and pigs (in vivo studies).

A 18F-labelled PET tracer for the in vivo imaging of cerebral A2AAR is part of our tracer development program in adenosinergic PET imaging (e.g. imaging of A1AR with [18F]CPFPX).