Competition [3H]NMS binding data for a range of mACh receptor antagonists in membrane homogenates prepared from CHO cells stably expressing either the wild-type or N410Y mutant M2 mACh receptor Data are expressed as mean (S.E.M.) values from n ≥ 3 experiments.
CHO-m2 Wild Type | CHO-m2 N410Y Mutant | |||||
|---|---|---|---|---|---|---|
| pKi | Hill Slope | pKi | Hill Slope | |||
| Atropine | 8.56 (0.05) | 1.07 (0.19) | 8.51 (0.06) | 0.99 (0.21) | ||
| Darifenacin | 7.57 (0.16) | 0.96 (0.03) | 6.78 (0.07)* | 1.01 (0.10) | ||
| Oxybutynin | 7.66 (0.03) | 1.05 (0.10) | 7.32 (0.07)* | 1.25 (0.26) | ||
| Tolterodine | 8.62 (0.05) | 1.01 (0.02) | 8.69 (0.06) | 1.01 (0.09) | ||
| Pirenzepine | 6.36 (0.05) | 0.97 (0.07) | 6.41 (0.02) | 0.91 (0.12) | ||
| Methoctramine | 8.31 (0.02) | 1.64 (0.10)** | 8.13 (0.16) | 1.40 (0.06)** | ||