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Chunk #25 — Adenosine, Receptors and Functions in the CNS — Adenosine A2AR and Functions in the CNS — [11C] PET radio ligands of adenosine A2AR

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Purinergic Receptors of the Central Nervous System: Biology, PET Ligands, and Their Applications.
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A2ARs with highest uptake in the putamen and the caudate, respectively.128 The lowest uptake of [11C]Preladenant was observed in the cerebellum. Estimated binding potential values of [11C]Preladenant with different scan durations were similar (4.3-5.3 in A2AR-rich regions).128 Preinjection with nonradiolabeled Preladenant reduced the tracer uptake in regions rich in A2AR and pretreatment with caffeine reduced tracer uptake in the striatum in a dose-dependent manner. [11C]Preladenant PET is a suitable tool to study A2AR occupancy in the brain.128 The regional distribution of [11C]Preladenant PET is consistent with known A2AR densities in the brain.126