Biochem/physiol Actions

ML184 (CID2440433) is a selective G-protein coupled receptor GPR55 (LPIR1) agonist (EC₅₀ = 0.26 µM vs. >32 µM toward GPR35 & CB1/2 by cell-based βarr2 recruitment assay; antagonist IC₅₀ = 15.1, 21.8, >32 µM, respectively, against CB2, CB1, GPR35). ML184 is 18-times more potent than lysophosphatidylinositol in stimulating cellular ERK1/2 phosphorylation (GPR55E- & βarr2-GFP-expressing U2OS cells) and is at least 10-times more potent than CID1792197 or CID1172084 (ML185) in inducing PKCβII translocation (GPR55E- & PKCβII-GFP-expressing HEK293 cells).