description | CID 16020046 is a GPR55 selective antagonist. It inhibits lpi-induced Ca2 + signaling, ERK1/2 phosphorylation, and gpr55-mediated activation of transcription factors. It has weak inhibitory effect on acetylcholinesterase, μ-opioid receptor, KCNH2 and hERG. It reduces the lpi-induced internalization of GPR55. |
biological activity | CID16020046 (C390-0219) is a selective GPR55 antagonist, which can inhibit the inherent activity of GPR55. IC50 is 0.15 μM in yeast. CID16020046 has only weak activity on other GPCRs, ion channels, kinases and nuclear receptors. |
target | TargetValue GPR55 (in east) 0.15 μM |
Target | Value |
GPR55
(in yeast)
| 0.15 μM |
In vitro study | In yeast cells expressing GPR55, CID16020046 can antagonize receptor activation induced by agonists. CID16020046 antagonized LPI-mediated calcium release and extracellular signal-regulated kinase activation in HEK293 cells stably expressing human GPR55, but not in HEK293 cells expressing CB1 or CB2. CID16020046 concentration-dependent inhibition of LPI-induced activation of NFAT, NF-κB and serum response elements, inhibition of NFAT and NF-κB translocation and internalization of GPR55. |
in vivo study | in intestinal inflammation model, CID16020046 improve inflammatory response and reduce pro-inflammatory cytokines. CID16020046 did not change the exercise and anxiety behaviors of healthy mice. |