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Ogerin is a potent and selective small-molecule allosteric agonist of the G protein-coupled receptor 68 (GPR68), also known as ovarian cancer G protein-coupled receptor 1 (OGR1). GPR68 is a proton-sensing receptor that is activated by extracellular acidity and is involved in various physiological processes, including pH homeostasis, inflammation, and bone metabolism. Ogerin was discovered through a yeast-based high-throughput screen of the pharmacologically dark G protein-coupled receptors. It has been utilized as a chemical probe to investigate the role of GPR68 in the central nervous system, where it has been shown to modulate fear conditioning and hippocampal-dependent learning in mice. Ogerin demonstrates high selectivity for GPR68 over other closely related proton-sensing receptors such as GPR4, GPR65, and GPR174.
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