JNJ-63533054 (1802326-66-4) is a potent and selective brain-penetrant GPR139 agonist (EC50=16 nM) an orphan G-protein-coupled receptor expressed in the CNS.1?Tritium-labeled JNJ-63533054 binds to cell membranes expressing GPR139 and can be displaced by putative endogenous ligands.2?Decreases compulsive-like alcohol drinking and hyperalgesia in alcohol-dependent rodents.3?Suppresses morphine intake in a mouse self-administration model.4
