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The G-protein-coupled receptor (GPCR) superfamily is comprised of an estimated 600-1,000 members and is the largest known class of molecular targets with proven therapeutic value. GPR18 is an orphan G protein-coupled receptor found at high levels in the testis, small intestines and cells associated with the immune system including lymphocytes, thymus and spleen. GPR18 has been found to be a receptor for endogenous lipid neurotransmitters, several of which also bind to cannabinoid receptors. Some ligands described to be GPR18 agonists or partial agonists include N-Arachidonoylglycine, Abnormal cannabidiol, O-1602, AM-251, Cannabidiol, delta 9-Tetrahydrocannabinol, N-arachidonoyl ethanolamine and Arachidonylcyclopropylamide. Antagonists include the synthetic cannabidiol related compounds CID-85469571 and O-1918.
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