Potencies and efficacies of CP55940 and LY2828360 in internalization, cyclase, and pERK1/2 assays at human CB2 receptors
Duration of drug incubation is expressed in minutes. cAMP accumulation assays were performed in duplicate. All other assays were performed in triplicate. EC50, 95% confidence intervals (CI), and the maximal effect (Emax, mean ± S.E.M.) were obtained by plotting and analyzing the data using GraphPad Prism 4.
| CP55940 | LY2828360 | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Drug Incubation | EC50 | 95% CI | Emax | ± S.E.M. | EC50 | 95% CI | Emax | ±S.E.M. | |
| Internalization | min 90 | nM 3 | 0.3–15.6 | % 33.9 | ±4.6 | nM ND | ND | % 10.2 | ±7.1 |
| Cyclase | 05 | 12.3 | 2.9–18.3 | 59.6 | ±8.3 | ND | ND | ND | ND |
| 35 | — | — | — | — | 16.7 | 4.6–59.6 | 42.8 | ±2.7 | |
| pERK1/2 | 05 | 3.77 | 0.4–12.7 | 95.7 | ±9.1 | ND | ND | 22.1 | ±5.8 |
| 30 | 23.3 | 10.1–53.9 | 49.4 | ±1.6 | 33.5 | 9.1–107.1 | 32.3 | ±1.9 | |
ND, Not determined or cannot be determined.