TABLE 1.
Apparent affinity values for VU0255035 and atropine for the competition of [3H]NMS binding from M1-M5 mAChRs
Ki values of VU0255035 and atropine were determined based on competition binding experiments with 0.1 nM [3H]NMS at each mAChR. The data represent the mean of three independent experiments performed in triplicate, and error bars represent S.E.M.
| VU0255035 Ki | -Fold Selectivity (vs M1) | Atropine Ki | |
|---|---|---|---|
| nM | nM | ||
| M1 | 14.87 ± 0.66 | 0.80 ± 0.07 | |
| M2 | 661.33 ± 57.64 | 45 | 2.60 ± 0.18 |
| M3 | 876.93 ± 151.44 | 59 | 1.09 ± 0.02 |
| M4 | 1177.67 ± 124.42 | 79 | 0.55 ± 0.31 |
| M5 | 2362.33 ± 577.49 | 159 | 1.64 ± 0.17 |