Relationship between side effects of antiparkinsonian agents and dopaminergic regulatory mechanism of adenosine receptors measured with PET

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Adenosine A^<2A> receptors (A2ARs) are thought to interact negatively with the dopamine D_2 receptor (D2R). We developed PET ligands for mapping adenosine receptors, and we successfully visualized A2ARs with ^<11>C-TMSX. In this study, we investigated A2ARs in the striata of drug-naive PD patients and PD patients with dyskinesia using ^<11>C-TMSX PET. Our study demonstrated that the A2ARs in the putamen were increased in the PD patients with dyskinesia, and also suggested that the A2ARs in the putamen compensate for the asymmetrical decrease of dopamine in drug-naive PD patients and that antiparkinsonian therapy increases the A2ARs in the putamen. The A2ARs may play an important role in regulation of parkinsonism in PD.