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N-Arachidonylglycine (NA-Gly), a carboxylic analog of the endocannabinoid anandamide (AEA), is a GPR18 agonist (EC₅₀ = 44.5 nM). Unlike AEA, N-Arachidonylglycine has no activity at either CB1 or CB2 receptors. N-Arachidonylglycine inhibits GLYT2 (IC₅₀ = 5.1 μM). N-Arachidonylglycine also is an effective activator of endometrial cell migration.

N-Arachidonylglycine (0.1 nM-100 µM; 5 min) drives MAPK activation in GPR18-transfected HEK293 cells.
N-Arachidonylglycine shows no activity at GLYT1 or GAT1 at concentrations up to 100 μm.

N-Arachidonylglycine (10 mg/kg; oral) increases blood concentrations of anandamide 9-fold.
N-Arachidonylglycine (1.2 mg/kg; oral; once) results in a significant 70% reduction of peritoneal cells.

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