Antagonist inhibition of Gαq-induced (constitutive) and agonist-induced activity
| Antagonist | pKi (% inhibition) | pKi | pKi | |||
|---|---|---|---|---|---|---|
| m1 + Cch | m1 + GQ | m3 + Cch | m3 + GQ | m5 + Cch | m5 + GQ | |
| Atropine | 8.78 ± 0.45 | 8.66 ± 0.33 | 9.11 ± 0.68 | 8.99 ± 0.23 | 8.66 ± 1.10 | 9.00 ± 0.40 |
| (100%) | (100%) | (100%) | (100%) | (100%) | (100%) | |
| Pirenzepine | 7.40 ± 0.42 | 7.64 ± 0.18 | 6.69 ± 0.13 | 6.83 ± 0.11 | 6.65 ± 0.36 | 7.03 ± 0.47 |
| (108 ± 13%) | (84 ± 31%) | (109 ± 2%) | (72 ± 10%) | (98 ± 22%) | (86 ± 8%) | |
| N-methyl scopolamine | 9.39 ± 0.05 | 9.49 ± 0.26 | 9.70 ± 0.45 | 9.57 ± 0.21 | 8.82 ± 0.44 | 8.59 ± 0.07 |
| (104 ± 7%) | (101 ± 45%) | (105 ± 7%) | (121 ± 18%) | (94 ± 18%) | (82 ± 11%) | |
| QNB | 10.58 ± 0.20 | 10.71 ± 0.65 | 11.09 ± 0.68 | 10.71 ± 0.02 | 10.33 ± 0.06 | 11.04 ± 0.10 |
| (91 ± 11%) | (116 ± 45%) | (61 ± 37%) | (103 ± 4%) | (93 ± 8%) | (94 ± 17%) | |
| Trihexyphenidyl | 8.02 ± 0.27 | 8.22 ± 0.18 | 8.15 ± 0.38 | 7.91 ± 0.38 | 7.57 ± 0.18 | 7.48 ± 0.41 |
| (117 ± 21%) | (107 ± 30%) | (106 ± 29%) | (67 ± 15%) | (86 ± 14%) | (100 ± 19%) | |
| 4-Diphenylacetyoxy-N-methylperidine | 8.09 ± 0.11 | 8.33 ± 0.17 | 9.04 ± 0.17 | 9.08 ± 0.27 | 7.97 ± 0.24 | 8.11 ± 0.29 |
| (104 ± 16%) | (112 ± 22%) | (96 ± 3%) | (70 ± 30%) | (94 ± 5%) | (70 ± 5%) | |