GPR85 Receptor Antibodies
GPR85, also known as SREB2 (Super Conserved Receptor Expressed in Brain 2), is an orphan class A GPCR belonging to the SREB family together with GPR27 and GPR173. The receptor is predominantly expressed in the central nervous system, with particularly high expression in the thalamus, hippocampus, cerebral cortex, amygdala and other regions involved in cognition and emotional processing. GPR85 expression is relatively high during embryonic and early postnatal brain development and appears to be associated with neuronal differentiation and maturation. Although GPR85 has been proposed to couple to Gs proteins and regulate cAMP signaling, its endogenous signaling pathway and physiological ligand remain poorly characterized. Functional studies suggest that GPR85 acts as a negative regulator of neurogenesis and may influence neuronal proliferation, dendritic development, synaptic plasticity and learning and memory. GPR85 has attracted particular interest in schizophrenia and other neuropsychiatric disorders because genetic and animal studies have linked altered receptor expression to changes in brain morphology, neuronal development and behavioral phenotypes. GPR85 knockout mice show increased brain mass and enhanced neurogenesis, whereas GPR85 overexpression has been associated with reduced neuronal proliferation and schizophrenia-like neuroanatomical abnormalities. No endogenous ligand has been definitively identified, and GPR85 is not currently considered to exhibit significant constitutive activity under standard experimental conditions. Several synthetic inverse agonists, including compounds 2g, 3h and 3i, have been reported with approximately low-micromolar potency, but they lack sufficient selectivity and drug-like properties for therapeutic development. Consequently, no approved drug or clinical-stage GPR85-targeting compound currently exists, leaving GPR85 as an interesting but still poorly validated potential target for schizophrenia, cognitive disorders and other CNS diseases. For more information on GPR85 pharmacology please refer to the IUPHAR database. For further reading refer to:
Davenport AP, Alexander SP, Sharman JL, Pawson AJ, Benson HE, Monaghan AE, Liew WC, Mpamhanga CP, Bonner TI, Neubig RR, Pin JP, Spedding M, Harmar AJ. International Union of Basic and Clinical Pharmacology. LXXXVIII. G protein-coupled receptor list: recommendations for new pairings with cognate ligands. Pharmacol Rev. 2013 May 17;65(3):967-86. doi: 10.1124/pr.112.007179. PMID: 23686350; PMCID: PMC3698937.
Alexander SP, Battey J, Benson HE, Benya RV, Bonner TI, Davenport AP, Dhanachandra Singh K, Eguchi S, Harmar A, Holliday N, Jensen RT, Karnik S, Kostenis E, Liew WC, Monaghan AE, Mpamhanga C, Neubig R, Pawson AJ, Pin JP, Sharman JL, Spedding M, Spindel E, Stoddart L, Storjohann L, Thomas WG, Tirupula K, Vanderheyden P. Class A Orphans in GtoPdb v.2023.1. IUPHAR/BPS Guide to Pharmacology CITE. 2023; 2023(1). Available from: https://doi.org/10.2218/gtopdb/F16/2023.1.