Operational model pKB and Schild slope estimates for McN-A-343, AC-42, and 77-LH-28-1 at the M2-WT and M2-EDGE-YT mAChRs from interaction studies with ACh in assays of ERK1/2 phosphorylation
Values represent the mean ± S.E.M. obtained from four to five experiments conducted in duplicate. pKB is the negative logarithm of the equilibrium dissociation constant, determined with the Schild slope constrained to equal 1
| M2-WT | M2-EDGE-YT | |||
|---|---|---|---|---|
| pKB | Schild Slope | pKB | Schild Slope | |
| McN-A-343 | 4.69 ± 0.10 | 1.19 ± 0.12 | N.P. | N.P. |
| AC-42 | 5.86 ± 0.11 | 0.92 ± 0.13 | 6.10 ± 0.13 | 1.15 ± 0.14 |
| 77-LH-28-1 | 5.95 ± 0.15 | 1.00 ± 0.16 | 6.44 ± 0.11* | 0.97 ± 0.13 |
N.P., not performed.
↵* Significantly different (P < 0.05) from the corresponding control value at the same receptor.