TABLE 1.
β-Arrestin-dependent ligand-mediated activation of GPR55E
CI, confidence interval.
| Ligand | GPR55 EC50 (95% CI) | Relative efficacy ± S.E. | CB1 (KI)a or EC50 |
|---|---|---|---|
| LPI | 1.2 μm (0.3–4.0), agonist | 1.0 ± 0.13 | No response up to 30 μm |
| SR141716A | 3.9 μm (0.9–17), agonist | 0.85 ± 0.15 | (3.3 nm)a (31), inverse agonist |
| AM251 | 9.6 μm (3.6–26), agonist | 1.21 ± 0.13 | (7.5 nm)a (31), inverse agonist |
| AM281 | No response up to 30 μm | (21 nm)a (31), inverse agonist | |
| 2-AG | No response up to 30 μm | 30 nm (42), agonist | |
| Anandamide | No response up to 30 μm | 116 nm, agonistb | |
| Palmitoyl ethanolamide | No response up to 30 μm | ||
| Methanandamide | No response up to 30 μm | ||
| THC | No response up to 30 μm | 6 nm (10), agonist | |
| HU210 | No response up to 30 μm | 70.2 pm (31), agonist | |
| CP55,940 | No response up to 30 μm | 1.2 nm (31), agonist | |
| O-1602 | No response up to 30 μm | >30,000 nm (10), agonist | |
| O-1918 | No response up to 30 μm | No binding (43) | |
| Abn-CBD | No response up to 30 μm | No binding (43) | |
| CBD | No response up to 30 μm | >30,000 nm (10), agonist | |
| SR144528 | No response up to 30 μm | (0.7 nm)a (44), CB2 antagonist | |
| WIN55212-2 | No response up to 30 μm | 5.5 nm (31), agonist | |
| JWH-015 | No response up to 30 μm | (13.8 nm) (45), CB2 agonist |
a
Previously published.
b
A. Kapur, P. Zhao, H. Sharir, Y. Bai, M. G. Caron, L. S. Barak, and M. E. Abood, unpublished information.