TABLE 4.
Transduction coefficients [Log10(τ/KA)], normalized (reference ligand ACh) transduction coefficients [ΔLog10(τ/KA)], and bias factors [ΔΔLog10(τ/KA)] for IP1 accumulation and phosphorylation of ERK1/2 at the wild-type M1 mAChR
| Compound | IP1 Accumulation |
ERK1/2
Phosphorylation |
Log Bias Factor
IP1 – ERK1/2 |
||
|---|---|---|---|---|---|
| Log10(τ/KA) | ΔLog10(τ/KA) | Log10(τ/KA) | ΔLog10(τ/KA) | ΔΔLog10(τ/KA) | |
| ACh | 7.10 ± 0.1 | 0.0 ± 0.1 | 7.1 ± 0.0 | 0.0 ± 0.0 | 0.0 ± 0.1 |
| Xanomeline | 8.2 ± 0.1 | 1.1 ± 0.1 | 7.1 ± 0.3 | 0.0 ± 0.3 | 1.1 ± 0.1 |
| GSK1034702 | 7.4 ± 0.2 | 0.3 ± 0.2 | 7.2 ± 0.1 | 0.1 ± 0.1 | 0.2 ± 0.2 |
| TBPB | 8.2 ± 0.2 | 1.1 ± 0.2 | 6.9 ± 0.4 | −0.3 ± 0.4 | 1.4 ± 0.2 |