Adenosine receptors (ARs) are a class of purinergic G-protein-coupled receptors (GPCRs).
Extracellular adenosine is a pivotal regulation molecule that adjusts physiological function through the
interaction with four ARs: A1R, A2AR, A2BR, and A3R. Alterations of ARs function and expression have
been studied in neurological diseases (epilepsy, Alzheimer’s disease, and Parkinson’s disease), cardiovascular
diseases, cancer, and inflammation and autoimmune diseases. A series of Positron Emission
Tomography (PET) probes for imaging ARs have been developed. The PET imaging probes have provided
valuable information for diagnosis and therapy of diseases related to alterations of ARs expression.
This review presents a concise overview of various ARs-targeted radioligands for PET imaging in
diseases. The most recent advances in PET imaging studies by using ARs-targeted probes are briefly
summarized.
