CID 16020046

CID16020046 is a selective GPR55 inverse agonist. CID16020046 is a G protein-coupled receptor that is weakly activated by some cannabinoids at nM concentrations. CID16020046 has been shown to block GPR55-mediated endothelial wound healing and reverse LPI-inhibited platelet aggregation. (In Vitro) :CID 16020046 has weak activities close for inhibition of the acetylcholinesterase (pIC50=4.4), antagonism of the m-opioid receptor (pIC50=4.6), and blockade of KCNH2, the hERG channel (pIC50=4.6) 6 in human embryonic kidney (HEK) -G protein–coupled receptor 55 (GPR55) cells.CID 16020046 (2.5 μM; for ≥25 minutes) significantly inhibits the lysophosphatidylinositol (LPI; 2.5 μM) induced ERK1/2 phosphorylation. CID 16020046 alone fails to induce intracellular Ca2+ release in HEK-GPR55, HEKCB1 cells and shows no ERK1/2 phosphorylation.Pretreatment with CID16020046 (0.01, 0.1, 1, 10 μM) leads to a concentration-dependent decrease in GPR55-mediated NFAT activation, NF-kB activation, and SRE induction in response to 1 μM LPI or GSK319197A in HEKGPR55 and HEK-CB1 cells.CID16020046 (2.5 μM) antagonizes GPR55-mediated activation and nuclear translocation of transcription factors but has no effect on CB1-mediated CREB activation.Pretreatment CID16020046 (1 μM) abolished the LPI-induced stimulation of wound healing in HMVEC-Ls.