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.
体外研究
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.
Western Blot Analysis
Cell Line:
HEK293-GPR18 cells
Concentration:
0.1 nM-100 µM
Incubation Time:
5 min
Result:
Drove MAPK activation.
体内研究
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.
Animal Model:
Rats
Dosage:
10 mg/kg
Administration:
Oral
Result:
Inhibition of FAAH, causing a reduction in the hydrolytic cleavage of anandamid.
Animal Model:
Mouse (peritonitis model)
Dosage:
1.2 mg/kg
Administration:
Oral; once
Result:
Resulted in a significant 70% reduction of peritoneal cells.
分子式
C22H35NO3
分子量
361.52
CAS号
179113-91-8
运输条件
Room temperature in continental US; may vary elsewhere.