M1/M4 receptor selectivity for agonists
| Max. | EC50 (nM) | log(max/EC50) | pEC50 | Δlog(max/EC50) | Rel. Aga | ΔpEC50 | Rel. Ag.b | |
|---|---|---|---|---|---|---|---|---|
| Relative agonism at M1 receptors Acetylcholine | 1 | 25.7 | 7.59 | 7.59 | 0 | 1 | 0 | 1 |
| Sabcom. | 0.389 | 56.2 | 6.84 | 7.25 | −0.75 | 0.178 | −0.34 | 0.457 |
| Talsaclidinec | 0.693 | 812.8 | 5.93 | 6.09 | −1.66 | 0.022 | −1.5 | 0.032 |
| Xanol | 0.637 | 43.7 | 7.16 | 7.36 | −0.43 | 0.375 | −0.23 | 0.589 |
| Relative agonism at M4 receptors | ||||||||
| Acetylcholine | 0.87 | 52.5 | 7.22 | 7.28 | 0 | 1 | 0 | 1 |
| Sabcom | 0.2 | 67.6 | 6.47 | 7.17 | −0.75 | 0.178 | −011 | 0.776 |
| Talsaclidine | 0.216 | 794.3 | 5.43 | 6.1 | −1.79 | 0.016 | −1.18 | 0.066 |
| Xanol | 0.46 | 63.1 | 6.86 | 7.2 | −0.36 | 0.44 | −0.08 | 0.832 |
↵a Relative agonism based on log(max/EC50) values.
↵b Relative agonism based on EC50 values.
↵c Talsaclidine selectivity was calculated as ΔΔlog(max/EC50). ΔΔLog(max/EC50) = 0.13: Talsaclidine is 100.13 = 1.38 selective for M1 receptors. Talsaclidine selectivity calculated as ΔΔpEC50. ΔΔpEC5 = −0.32: Talsaclidine is 10−0.32 = 0.48 selective for M1 receptors (i.e., 2.1 × selective for M4 receptors).
Data from Watt et al., 2011.