Concentration-effect data for agonist stimulation of [35S]GTPγS of wild-type and mutant receptors expressed in HEK 293 cells
Data represent the mean of at least three independent experiments performed in triplicate. EC50 values were determined from concentration-effect curves using Prism software. The values in parentheses are the 95% confidence intervals (CI). Statistical analysis was performed by comparing the log EC50 of the mutant receptor with that of the wild-type CB1 receptors using the Student t test to determine the level of significance.
Agonist & Cell Line | EC50 (CI) | Mutant/WT EC50 |
|---|---|---|
| WIN55,212-2 | ||
| WT | 5.5 nM (1-30) | 1 |
| S7.39A | 14.7 nM (4-53) | 2.6 |
| S2.60A | 27 nM (5-140) | 4.8 |
| CP55,940 | ||
| WT | 0.75 nM (0.3-1.7) | 1 |
| S7.39A | N.D. | |
| S2.60A | 3.8 nM (1-15) | 5 |
| HU210 | ||
| WT | 70.2 pM (22.4-220) | 1 |
| S7.39A | 13.9 nM (2.5-76)* | 198 |
| S2.60A | 317 pM (42-2300) | 4.5 |
| AM4056 | ||
| WT | 26.8 pM (4-170) | 1 |
| S7.39A | 15.6 nM (6.7-36)** | 580 |
| S2.60A | 33.4 pM (3.3-300) | 1.2 |