Table 3. Potency and efficacy (as % of acetylcholine response) of muscarinic agonists at WT and mutated M1 receptors.
| Compound | hM1-WT | hM1-Y381A |
|---|---|---|
| Acetylcholine | 21 ± 6 (100) | 3,837 ± 677 (100) |
| Carbachol | 76 ± 18 (96 ± 1) | 12,538 ± 2,496 (93 ± 3) |
| Clozapine | 293 ± 87 (11 ± 1) | 15 ± 2 (90 ± 1) |
| N-desmethylclozapine | 115 ± 28 (50 ± 5) | 14 ± 2 (96 ± 2) |
| AC42 | 805 ± 251 (71 ± 2) | 220 ± 16 (83 ± 3) |
C50 values (nM) are mean ± SEM of three determinations. Numbers in parentheses are percentage of acetylcholine response.