NAGly receptor
Template:PBB 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
- Agonists
Ligands found to bind to GPR18 as agonists include:[6][8]
- N-arachidonoyl glycine (NAGly)
- Abnormal cannabidiol (Abn-CBD)
- AM-251 - partial agonist
- Cannabidiol - partial agonist
- O-1602
- Δ9-Tetrahydrocannabinol (Δ9-THC) - THC is actually a more potent agonist at GPR18 than at CB1 or CB2, with Ki of 0.96nM at GPR18, 8.1nM at GPR55, 25.1nM at CB1 and 35.2nM at CB2.[9]
- Anandamide (N-arachidonoyl ethanolamine, AEA)
- Arachidonylcyclopropylamide (ACPA) [10]
- Antagonists
References
- ^ 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.
{{cite journal}}: Explicit use of et al. in:|author=(help) - ^ "Entrez Gene: GPR18 G protein-coupled receptor 18".
- ^ 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.
{{cite journal}}: Explicit use of et al. in:|author=(help) - ^ 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.
- ^ 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.
{{cite journal}}: CS1 maint: multiple names: authors list (link) - ^ 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.
{{cite journal}}: Explicit use of et al. in:|author=(help)CS1 maint: unflagged free DOI (link) - ^ Lu, VB (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.
{{cite journal}}: Unknown parameter|coauthors=ignored (|author=suggested) (help) - ^ 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.
{{cite journal}}: CS1 maint: multiple names: authors list (link) - ^ Attention: This template ({{cite pmid}}) is deprecated. To cite the publication identified by PMID 22831390, please use {{cite journal}} with
|pmid=22831390instead. - ^ Attention: This template ({{cite doi}}) is deprecated. To cite the publication identified by doi:10.1007/978-1-4614-4669-9_6, please use {{cite journal}} (if it was published in a bona fide academic journal, otherwise {{cite report}} with
|doi=10.1007/978-1-4614-4669-9_6instead.
Further reading
- Christian SL; et al. (2002). "An evaluation of the assembly of an approximately 15-Mb region on human chromosome 13q32-q33 linked to bipolar disorder and schizophrenia". Genomics. 79 (5): 635–56. doi:10.1006/geno.2002.6765. PMID 11991713.
{{cite journal}}: Explicit use of et al. in:|author=(help) - Strausberg RL; et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. doi:10.1073/pnas.242603899. PMC 139241. PMID 12477932.
{{cite journal}}: Explicit use of et al. in:|author=(help) - Dunham A; et al. (2004). "The DNA sequence and analysis of human chromosome 13". Nature. 428 (6982): 522–8. doi:10.1038/nature02379. PMC 2665288. PMID 15057823.
{{cite journal}}: Explicit use of et al. in:|author=(help) - Gerhard DS; et al. (2004). "The Status, Quality, and Expansion of the NIH Full-Length cDNA Project: The Mammalian Gene Collection (MGC)". Genome Res. 14 (10B): 2121–7. doi:10.1101/gr.2596504. PMC 528928. PMID 15489334.
{{cite journal}}: Explicit use of et al. in:|author=(help) - Kohno M; et al. (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.
{{cite journal}}: Explicit use of et al. in:|author=(help)
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