Table 1.
Ligand potencies in various assays on GPR55-HEK cells (EC50 µM)
| Ligand | Ca2+microfluorimetry | NFAT-activation | ERK phosphorylation |
|---|---|---|---|
| LPI | 0.049 ± 0.004 | 1.10 ± 0.02 | 0.074 ± 0.013 |
| AM251 | 0.63 ± 0.11 | 1.13 ± 0.07 | 0.54 ± 0.15 |
| SR141716A | 1.14 ± 0.03 | >1 | 0.64 ± 0.25 |
| AM281 | 13.6 ± 3.30 | 13.1 ± 0.8 | >3 |
| CREB-phosphorylation | NF-κB activation | EPIC DMR | |
| LPI | 0.093 ± 0.01 | 1.9 ± 0.04 | 0.009 ± 0.0001 |
| AM251 | 0.43 ± 0.09 | >0.5 | 0.81 ± 0.14 |
| SR141716A | 0.48 ± 0.05 | >1 | 1.85 ± 0.1 |
| AM281 | >3 | 7.25 ± 0.23 | 4.1 ± 0.09 |
Data are means ± SEM (n= 2–5).
CREB, cAMP response element binding protein; DMR, dynamic mass redistribution; ERK, extracellular signal regulated kinase; GPR55-HEK293, stable HEK293 cells expressing 3xHA-GPR55; LPI, L-α-lysophosphatidylinositol; NFAT, nuclear factor of activated T cells; NF-κB, nuclear factor-κB.