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Chunk #40 — 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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Some P2X7 receptor antagonists were specifically developed to study disorders of the CNS. These are the brain penetrant benzamides GSK1482160,196 JNJ-42253432,197 JNJ-47965567,198 triazoles JNJ-54232334 and JNJ-54140515,199 JNJ-54166060,200 JNJ-54173717,201 JNJ-54175446,202 and JNJ-55308942.203 These molecules have demonstrated P2X7 receptor antagonist activities in rodent and human. Three of these molecules, GSK1482160, JNJ-54175446, and JNJ-55308942, have already moved into clinical trials for evaluation of the disorders of CNS.187