Potency (pEC50) estimates for inhibition of G protein activity by 2A3BTs in [35S]GTPγS binding assay at the M2 mAChR (n = 4) and A1 receptor (n = 3)
| pEC50 | |||
|---|---|---|---|
| M2 mAChR | A1R | ||
| +10 μM Atropine | +100 μM Carbachol | +10 μM DPCPX | |
| LUF5484 | 5.33 ± 0.22 | 5.53 ± 0.06 | N.D. |
| PD81,723 | 4.98 ± 0.25 | 4.97 ± 0.07 | N.D. |
| T62 | 5.68 ± 0.26 | 5.60 ± 0.10 | 5.23 ± 0.08 |
| VCP520 | 5.78 ± 0.21 | 5.78 ± 0.08 | N.A. |
| VCP333 | 5.77 ± 0.25 | 5.60 ± 0.07 | 5.67 ± 0.13 |
N.D., not determined; N.A., not applicable.