A positive allosteric modulator of GPR68
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Ogerin is a positive allosteric modulator of G protein-coupled receptor 68 (GPR68).1 It increases proton-induced cAMP production in HEK293T cells expressing the human receptor in a reporter assay. Ogerin inhibits proton-mediated calcium release in the same cells when used at a concentration of 10 ?M. It impairs contextual, but not cued, fear conditioning in wild-type, but not Gpr68 knockout, mice when administered at a dose of 10 mg/kg.
1.Huang, X.-P., Karpiak, J., Kroeze, W.K., et al.Allosteric ligands for the pharmacologically dark receptors GPR68 and GPR65Nature527(7579)477-483(2015)
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