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Chunk #41 — P2X Receptors and Functions in the CNS — P2X7 Receptor and Functions in the CNS

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Purinergic Receptors of the Central Nervous System: Biology, PET Ligands, and Their Applications.
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Association of P2X7R activation with pro-inflammatory phenotype of microglia in CNS diseases makes P2X7R an interesting and valuable biomarker of inflammation.9 Development of useful PET radioligands for imaging the P2X7Rs in CNS can potentially enable studies of the pharmacology and functional role of this receptor in neuroinflammation and evaluate the effect of therapeutic agents in treating neuroinflammatory and neurodegenerative diseases. Fortunately, an ample number of potent and selective P2X7R ligands has presented opportunities to develop a few 11C and 18F PET radioligands of the receptor as described herein.24,204