GPR45 Receptor Antibodies

GPR45 is an orphan class A G protein-coupled receptor with 372 amino acids for which no endogenous ligand has yet been conclusively identified. Pharmacologically, GPR45 remains poorly characterized, although experimental studies indicate coupling to both Gs- and Gi/o-family G proteins, suggesting that it may regulate intracellular cAMP signaling. The receptor is expressed predominantly in the central nervous system, including the basal forebrain, frontal cortex and several neuronal populations such as cortical, hippocampal, olfactory and cerebellar neurons, but expression has also been detected in peripheral tissues including the liver. GPR45 expression is already detectable during embryonic brain development and persists into adulthood, suggesting a role in neuronal function and homeostasis. Recent genetic studies have identified GPR45 as an important regulator of energy balance, as deletion of Gpr45 in mice causes increased food intake, obesity, increased adiposity, insulin resistance and hepatic steatosis. More detailed studies indicate that GPR45-expressing neurons in the paraventricular hypothalamus are involved in suppression of food intake and regulation of body weight. These findings have generated considerable interest in GPR45 as a potential therapeutic target for obesity and metabolic disease. However, the precise endogenous signaling pathway and physiological ligand of GPR45 remain unknown, and there are currently no validated selective small-molecule agonists or antagonists. Consequently, no approved drug or clinical-stage compound targeting GPR45 is currently available, making it an interesting but still largely unexplored pharmacological target for metabolic disease and potentially CNS disorders. For more information on GPR45 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.