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Ogerin is a potent GPR68 modulator.
Biochem/physiol Actions
Ogerin is a selective positive allosteric modulator of an orphan GPCR, GPR68, also known as Ovarian cancer G-protein coupled receptor 1 (OGR1). GPR68 is one of the proton or pH-sensing GPCRs that sense extracellular H(+). Ogerin potently potentiated proton-mediated GPR68-Gs signaling. Ogerin was not active in GPR68 knockout mice, but was found to suppress recall in fear conditioning in wild-type mice, showing an unexpected effect of GPR68 on learning and memory.
酵素阻害剤
This GPR68 activator (FW = 307.35 g/mol; CAS 1309198-71-7), also named 2-[4-amino-6-[(phenylmethyl)amino]-1,3,5-triazin-2-yl]benzenemethanol, selectively and allosterically targets G-Protein-coupled Receptor 68, one of at least 120 non-olfactory G-protein-coupled receptors in the human genome that remain 'orphans' (i.e., they are pharmacologically dark, with no known endogenous ligands). Ogerin suppresses recall in fear conditioning in wild-type, but not in GPR68-knockout mice. GPR68 is also a newly recognized metastasis suppressor gene in certain cancers.
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