URB602 explained

URB602 ([1,1'-biphenyl]-3-yl-carbamic acid, cyclohexyl ester) is a compound that has been found to inhibit hydrolysis of monoacyl glycerol compounds, such as 2-arachidonoylglycerol (2-AG) and 2-oleoylglycerol (2-OG). It was first described in 2003.^[1] A study performed in 2005 found that the compound had specificity for metabolizing 2-AG over anandamide (another cannabinoid ligand) in rat brain presumably by inhibiting the enzyme monoacylglycerol lipase (MAGL), which is the primary metabolic enzyme of 2-AG.^[2] However, subsequent studies have shown that URB602 lacks specificity for MAGL inhibition in vitro.^[3]

Notes and References

1. Tarzia . G . Duranti . A . Tontini . A . Piersanti . G . Mor . M . Rivara . S . Plazzi . PV . Park . C . Kathuria . S . Piomelli . Daniele . Design, synthesis, and structure-activity relationships of alkylcarbamic acid aryl esters, a new class of fatty acid amide hydrolase inhibitors . Journal of Medicinal Chemistry . 46 . 12 . 2352–60 . 2003 . 12773040 . 10.1021/jm021119g. 30528443 . 8 .
2. Hohmann . Andrea G. . Suplita . Richard L. . Bolton . Nathan M. . Neely . Mark H. . Fegley . Darren . Mangieri . Regina . Krey . Jocelyn F. . Michael Walker . J. . Holmes . Philip V. . Crystal . Jonathon D. . Duranti . Andrea . Tontini . Andrea . Mor . Marco . Tarzia . Giorgio . Piomelli . Daniele . An endocannabinoid mechanism for stress-induced analgesia . Nature . 435 . 7045 . 1108–12 . 2005 . 15973410 . 10.1038/nature03658 . 2005Natur.435.1108H. 4339948 . 8 .
3. Vandevoorde . S . Jonsson . K-O . Labar . G . Persson . E . Lambert . D M . Fowler . C J . Lack of selectivity of URB602 for 2-oleoylglycerol compared to anandamide hydrolysisin vitro . British Journal of Pharmacology . 150 . 2 . 186–91 . 2007 . 17143303 . 2042901 . 10.1038/sj.bjp.0706971.