2140803-86-5

ML193 is a potent and selective piperadinyloxadiazolone antagonist for G protein-coupled receptor (GPCR) GPR55a receptor for L-α-lysophosphatidylinositol (LPI) which also binds synthetic cannabinoidsand signals through several endogenous pathways. GPR55 is highly abundant in the CNS as well as in intestinebone marrowspleenplateletsimmune and endothelial cells. Its role is not completely understoodbut has been implicated in inflammatory painneuropathic painmetabolic disorderbone developmentand cancer. Selective antagonists are needed to further elucidate the role of GPR55 in physiology and pathobiology. ML193 (CID1261822) has 221 nM potency for GPR55 and >145-fold>27-fold and >145-fold antagonist selectivity against GPR35cannabinoid receptors CB1 and CB2respectively and >145-fold agonist selectivity against GPR35CB1 and CB2. ML193 is inhibits the downstream responses of ERK phosphorylation with an IC50 of 65 nM and PKC ^