Concentration-response curve potency (pEC50) and maximal agonist response (Emax) parameters for agonist-stimulated phosphorylation of ERK1/2 at the WT and DREADD M4 mAChR
Values represent the mean ± S.E.M. from n experiments performed in triplicate.
Ligand | M4 WT | M4 DREADD | n | ||||
|---|---|---|---|---|---|---|---|
| pEC50 | Emax | pEC50 | Emax | ||||
| ACh | 7.6 ± 0.1 | 74 ± 2 | 2.7 ± 0.4* | 23 ± 5* | 7 | ||
| Pilocarpine | 5.7 ± 0.3 | 40 ± 4 | N.D. | N.D. | 4 | ||
| McN-A-343 | 6.7 ± 0.1 | 53 ± 3 | N.D. | N.D. | 7 | ||
| LY2033298 | 7.0 ± 0.1 | 55 ± 2 | N.D. | N.D. | 7 | ||
| Clozapine | N.D. | N.D. | 8.4 ± 0.1 | 53 ± 1 | 7 | ||
| CNO | N.D. | N.D. | 7.0 ± 0.1 | 45 ± 2 | 7 | ||
| NDMC | 6.8 ± 0.7 | 19 ± 3 | 8.0 ± 0.1* | 42 ± 1* | 7 | ||
pEC50, negative logarithm of the EC50; Emax, maximal agonist-stimulated response, expressed as a percentage of the response stimulated by 10% FBS;, N.D., not determined.
↵* Significantly different (P < 0.05) from the corresponding parameter at the M4 WT, as determined by Student's t test.