Neuropeptides B/W receptor 1, also known asNPBW1 and formerly asGPR7, is a humanprotein encoded by theNPBWR1gene.[5] As implied by its name, it and related gene NPBW2 (with which it shares 70%nucleotide identity) aretransmembranes protein that bindNeuropeptide B (NPB) andNeuropeptide W (NPW), both proteins expressed strongly in parts of the brain that regulate stress and fear including the extendedamygdala andstria terminalis. When originally discovered in 1995, these receptors had no knownligands ("orphan receptors") and were called GPR7 and GPR8,[6] but at least three groups in the early 2000s independently identified their endogenous ligands, triggering the name change in 2005.[7]
In rodent models, NPBWR1 is over-expressed inSchwann cells associated withneuropathic pain, suggesting it inhibits inflammatory pain responses.[10] Mice without NPBW1 exhibited a stronger hostile reaction to intruders, suggesting NPBW1 has a role instress responses.[11] Early studies indicated that NPB and NPW had a complex effect on appetite, but generally led toanorexia.[12] Similarly, male rats lacking NPBWR1 exhibitedhyperphagia and adult-onsetobesity, though why female rats are unaffected is unknown.[13] Researchers speculated that activating these pathways might decrease obesity, and synthesized a small-molecule ligand that is capable of stimulating both receptors at low concentrations.[14]
^O'Dowd BF, Scheideler MA, Nguyen T, Cheng R, Rasmussen JS, Marchese A, et al. (1995). "The cloning and chromosomal mapping of two novel human opioid-somatostatin-like receptor genes, GPR7 and GPR8, expressed in discrete areas of the brain".Genomics.28 (1):84–91.doi:10.1006/geno.1995.1109.PMID7590751.
^Davenport A., Singh G. (2005). Neuropeptide W/Neuropeptide B Receptors – NPBW1. IUPHAR Receptor database.doi:10.1786/080844542445
^Hondo M, Ishii M, Sakurai T (2008). "The NPB/NPW neuropeptide system and its role in regulating energy homeostasis, pain, and emotion".Results Probl. Cell Differ. Results and Problems in Cell Differentiation.46:239–256.doi:10.1007/400_2007_056.ISBN978-3-540-78350-3.PMID18204824.
^Zaratin P, Quattrini A, Previtali S, Comi G, Hervieu G, Scheideler M (2005). "Schwann cell overexpression of the GPR7 receptor in inflammatory and painful neuropathies".Mol. Cell. Neurosci.28 (1):55–63.doi:10.1016/j.mcn.2004.08.010.PMID15607941.
^Romero FA, Hastings NB, Moningka R, Guo Z, Wang M, Di Salvo J, et al. (2012). "The discovery of potent antagonists of NPBWR1 (GPR7)".Bioorg. Med. Chem. Lett.22 (2):1014–1018.doi:10.1016/j.bmcl.2011.11.126.PMID22197390.
O'Dowd BF, Scheideler MA, Nguyen T, et al. (1995). "The cloning and chromosomal mapping of two novel human opioid-somatostatin-like receptor genes, GPR7 and GPR8, expressed in discrete areas of the brain".Genomics.28 (1):84–91.doi:10.1006/geno.1995.1109.PMID7590751.
Zaratin PF, Quattrini A, Previtali SC, et al. (2005). "Schwann cell overexpression of the GPR7 receptor in inflammatory and painful neuropathies".Mol. Cell. Neurosci.28 (1):55–63.doi:10.1016/j.mcn.2004.08.010.PMID15607941.S2CID40483027.
Cottrell S, Jung K, Kristiansen G, et al. (2007). "Discovery and validation of 3 novel DNA methylation markers of prostate cancer prognosis".J. Urol.177 (5):1753–8.doi:10.1016/j.juro.2007.01.010.PMID17437806.
