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GPR18 : ウィキペディア英語版
GPR18

''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. 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.
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,〔 though recent evidence demonstrates that NAGly was not shown to be a GPR18 agonist in rat sympathetic neurons.
==Ligands==
;Agonists
Ligands found to bind to GPR18 as agonists include:
* ''N''-Arachidonoylglycine (NAGly)
* Abnormal cannabidiol (Abn-CBD)
* AM-251 - partial agonist
* Cannabidiol - partial agonist
* O-1602
* Δ9-Tetrahydrocannabinol9-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.
* Anandamide (''N''-arachidonoyl ethanolamine, AEA)
* Arachidonylcyclopropylamide (ACPA)
* Resolvin D2 (RvD2)

;Antagonists
* O-1918
* CID-85469571 〔Rempel V, et al. Bicyclic imidazole-4-one derivatives: a new class of antagonists for the orphan G protein-coupled receptors GPR18 and GPR55. ''Med. Chem. Commun.'', 2014;5: 632-649. DOI 10.1039/C3MD00394A〕

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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