Estimated potency (pEC50) and maximal agonist effect (Emax) of mAChR agonists at mediating ERK1/2 phosphorylation
Values represent the mean ± S.E.M. obtained from 5 to 12 experiments performed in duplicate.
| M2-WT | M2-EDGE-YT | M2-EDGE | M2-YT | |
|---|---|---|---|---|
| Acetylcholine | ||||
| pEC50 | 7.52 ± 0.12 | 7.38 ± 0.12 | 7.64 ± 0.10 | 7.50 ± 0.09 |
| E max | 90.8 ± 6.1 | 105.3 ± 4.3 | 77.1 ± 6.1 | 89.3 ± 5.6 |
| Pilocarpine | ||||
| pEC50 | 6.16 ± 0.24 | 5.66 ± 0.06 | N.P. | N.P. |
| E max | 80.2 ± 5.6 | 108.3 ± 2.4* | N.P. | N.P. |
| McN-A-343 | ||||
| pEC50 | 5.35 ± 0.05 | 5.53 ± 0.12 | 5.10 ± 0.12 | 5.38 ± 0.11 |
| E max | 18.0 ± 4.1 | 97.1 ± 4.3* | 32.8 ± 8.1 | 68.0 ± 9.5* |
| AC-42 | ||||
| pEC50 | N.D. | N.D. | N.D. | N.D. |
| E max | N.D. | N.D. | N.D. | N.D. |
| 77-LH-28-1 | ||||
| pEC50 | 5.87 ± 0.05 | 6.98 ± 0.15* | 5.83 ± 0.53 | 6.78 ± 0.13* |
| E max | 16.8 ± 2.2 | 27.9 ± 4.7 | 13.43 ± 2.6 | 18.2 ± 3.0 |
N.D., value could not be accurately determined because of the very modest level of ERK1/2 phosphorylation; N.P., not performed
↵* Significantly different (p < 0.05) from the corresponding control value within the same treatment group.