JNJ-63533054 is a potent and selective brain-penetrant GPR139 agonist (EC50=16 nM) an orphan G-protein-coupled receptor expressed in the CNS. Tritium-labeled JNJ-63533054 binds to cell membranes expressing GPR139 and can be displaced by putative endogenous ligands. Decreases compulsive-like...
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JNJ-63533054 is a potent and selective brain-penetrant GPR139 agonist (EC50=16 nM) an orphan G-protein-coupled receptor expressed in the CNS. Tritium-labeled JNJ-63533054 binds to cell membranes expressing GPR139 and can be displaced by putative endogenous ligands. Decreases compulsive-like alcohol drinking and hyperalgesia in alcohol-dependent rodents. Suppresses morphine intake in a mouse self-administration model
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