GPR18

From Wikipedia, the free encyclopedia
Jump to: navigation, search
G protein-coupled receptor 18
Identifiers
Symbol GPR18
External IDs OMIM602042 MGI107859 HomoloGene18814 IUPHAR: GPR18 GeneCards: GPR18 Gene
RNA expression pattern
PBB GE GPR18 210279 at tn.png
More reference expression data
Orthologs
Species Human Mouse
Entrez 2841 110168
Ensembl ENSG00000125245 ENSMUSG00000050350
UniProt Q14330 Q8K1Z6
RefSeq (mRNA) NM_001098200 NM_182806
RefSeq (protein) NP_001091670 NP_877958
Location (UCSC) Chr 13:
99.91 – 99.91 Mb
Chr 14:
121.91 – 121.92 Mb
PubMed search [1] [2]

N-arachidonyl glycine receptor also known as G-protein coupled receptor 18 (GPR18) is a protein that in humans is encoded by the GPR18 gene.[1][2] Along with the other previously "orphan" receptors GPR55 and GPR119, GPR18 has been found to be a receptor for endogenous lipid neurotransmitters, several of which also bind to cannabinoid receptors.[3][4][5]

Research supports the hypothesis that GPR18 is the abnormal cannabidiol receptor and N-arachidonoyl glycine, the endogenous lipid metabolite of anandamide, initiates directed microglial migration in the CNS through activation of GPR18,[6] though recent evidence demonstrates that NAGly was not shown to be a GPR18 agonist in rat sympathetic neurons.[7]

Ligands[edit]

Agonists

Ligands found to bind to GPR18 as agonists include:[6][8]

Antagonists

References[edit]

  1. ^ Gantz I, et al. (Sep 1997). "Cloning and chromosomal localization of a gene (GPR18) encoding a novel seven transmembrane receptor highly expressed in spleen and testis". Genomics 42 (3): 462–6. doi:10.1006/geno.1997.4752. PMID 9205118. 
  2. ^ "Entrez Gene: GPR18 G protein-coupled receptor 18". 
  3. ^ Kohno M, et al. (September 2006). "Identification of N-arachidonylglycine as the endogenous ligand for orphan G-protein-coupled receptor GPR18". Biochem. Biophys. Res. Commun. 347 (3): 827–32. doi:10.1016/j.bbrc.2006.06.175. PMID 16844083. 
  4. ^ Burstein S (December 2008). "The elmiric acids: biologically active anandamide analogs". Neuropharmacology 55 (8): 1259–64. doi:10.1016/j.neuropharm.2007.11.011. PMC 2621443. PMID 18187165. 
  5. ^ Bradshaw HB, Lee SH, McHugh D (September 2009). "ORPHAN ENDOGENOUS LIPIDS AND ORPHAN GPCRS: A GOOD MATCH". Prostaglandins Other Lipid Mediat. 89 (3–4): 131–4. doi:10.1016/j.prostaglandins.2009.04.006. PMC 2740803. PMID 19379823. 
  6. ^ a b McHugh D, et al. (2010). "N-arachidonoyl glycine, an abundant endogenous lipid, potently drives directed cellular migration through GPR18, the putative abnormal cannabidiol receptor". BMC Neurosci 11: 44. doi:10.1186/1471-2202-11-44. PMC 2865488. PMID 20346144. 
  7. ^ Lu, VB; Puhl HL, 3rd; Ikeda, SR (Jan 2013). "N-Arachidonyl glycine does not activate G protein-coupled receptor 18 signaling via canonical pathways.". Molecular pharmacology 83 (1): 267–82. PMID 23104136. 
  8. ^ McHugh D, Page J, Dunn E, Bradshaw HB (May 2011). "Δ(9) -THC and N-arachidonyl glycine are full agonists at GPR18 and cause migration in the human endometrial cell line, HEC-1B". Br J Pharmacol 165 (8): no. doi:10.1111/j.1476-5381.2011.01497.x. PMID 21595653. 
  9. ^ Ashton, J. C. (2012). "The atypical cannabinoid o-1602: Targets, actions, and the central nervous system". Central nervous system agents in medicinal chemistry 12 (3): 233–239. doi:10.2174/187152412802430156. PMID 22831390.  edit
  10. ^ McHugh, D.; Bradshaw, H. B. (2013). "GPR18 and NAGly Signaling: New Members of the Endocannabinoid Family or Distant Cousins?". EndoCANNABINOIDS. p. 135. doi:10.1007/978-1-4614-4669-9_6. ISBN 978-1-4614-4668-2.  edit

Further reading[edit]