Potencies and efficacies of CP55940 and LY2828360 in arrestin, internalization, cyclase, and pERK1/2 assays at mouse CB2 receptors
Duration of drug incubation is expressed in minutes. All assays were performed in triplicates except cAMP accumulation assays, which were performed in duplicate. 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. | |
| Arrestin | min 90 | nM 2.3 | 0.4–12.2 | % 125 | ±1.6 | nM ND | ND | % 97.9 | ±1.5 |
| internalization | 90 | 7.4 | 1.1–19.3 | 49.1 | ±1.2 | 30.7 | 1.4–626.5 | 19.1 | ±2.4 |
| Cyclase | 05 | 6.6 | 1.7–12.2 | 52.8 | ±3.6 | ND | ND | 18.9 | ±5.8 |
| 30 | — | — | — | — | 13.6 | 10.4–45.3 | 53.4 | ±1.9 | |
| pERK1/2 | 05 | 10.5 | 2.2–17.9 | 136.2 | ±4.1 | ND | ND | 4.1 | ±2.5 |
| 20 | 1.5 | 0.1–3.7 | 20.3 | ±3.4 | 339 | 128.8–345.8 | 43.6 | ±2.3 | |
ND, Not determined or cannot be determined.