Functional activity of muscarinic agonists at wild-type M1, NC4M1M3, and NC3M1M3 chimeric receptors measured in calcium mobilization assays by FLIPR
EC50 values and percentage of maximum acetylcholine activity are presented as mean ± S.E.M. of three individual experiments performed in triplicate.
| hM1-WT | NC4M1M3 | NC3M1M3 | ||||
|---|---|---|---|---|---|---|
| EC50 | Max | EC50 | Max | EC50 | Max | |
| nM | % | nM | % | nM | % | |
| Acetylcholine | 5 ± 0.2 | 100 | 3.4 ± 1.5 | 100 | 40 ± 14 | 100 |
| Xanomeline | 3.2 ± 0.2 | 81 ± 3 | 18 ± 4 | 82 ± 2 | 44 ± 9 | 69 ± 5 |
| AC-42 | 128 ± 7 | 74 ± 1 | >100,000 | 922 ± 11 | 48 ± 3 | |
| TBPB | 5.3 ± 0.2 | 70 ± 0.4 | >100,000 | 117 ± 42 | 36 ± 4 | |
| N-desmethylclozapine | 20 ± 1 | 65 ± 0.4 | 59 ± 18 | 43 ± 2 | 83 ± 5 | 47 ± 3 |