The G protein-coupled receptor 55 (GPR55), a lysophosphatidylinositol (LPI) receptor that is responsive to certain cannabinoids, has been implicated in several (patho)physiologic functions. CID-16020046 (40 nM – 10 μM) acts as an inverse agonist, inhibiting GPR55 constitutive activity with an IC50 of 0.15 μM. In HEK-GPR55 cells, pretreatment with increasing concentrations of CID-16020046 inhibited GPR55 agonist-induced intracellular Ca2+ release. Further, 2.5 μM CID-16020046 significantly inhibited the LPI (a GPR55 agonist)-induced ERK1/2 phosphorylation, GPR55 internalization and GPR55-mediated transcription factor activation in HEK-GPR55 cells[3]. In the DSS (dextran sulfate sodium) and TNBS (trinitrobenzene sulfonic acid) colitis models, treatment with CID-16020046 at a dosage of 20 mg/kg significantly reduced macroscopic scores and MPO (myeloperoxidase) activity as compared to vehicle-treated animals[4].
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