TABLE 1.
Estimates of potency (pEC50) and maximal effect (Emax) of agonists mediating ERK1/2 phosphorylation at the indicated M2 mAChR in the absence or presence of DDBL-4 Values represent the mean ± S.E. obtained from three to six experiments conducted in duplicate.
|
M2 mAChR (wild type)
|
M2 mAChR (Y177A)
|
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|---|---|---|---|---|---|---|---|---|
|
Control
|
100 μm DDBL-4
|
Control
|
100 μm DDBL-4
|
|||||
| pEC50 | Emaxa | pEC50 | Emax | pEC50 | Emaxa | pEC50 | Emax | |
| Ach | 7.83 ± 0.09 | 87.09 ± 2.31 | 6.82 ± 0.09b | 61.46 ± 2.21b | 8.18 ± 0.09 | 86.50 ± 1.65 | 80.71 ± 2.87 | |
| TMA | 4.01 ± 0.09 | 75.83 ± 3.03 | 3.71 ± 0.07b | 44.22 ± 1.43b | 4.51 ± 0.13 | 82.91 ± 3.46 | 4.11 ± 0.24 | 61.26 ± 5.39b |
a
Parameter normalized to the maximum response elicited by 3% FBS
b
Significantly different (p < 0.05) from corresponding control value (Student's t test)