| No recycle | 3 h recycle |
---|
No drug
| 100 | 100 |
Carbachol
| 48 ± 4* | 102 ± 10 |
Oxotremorine-M
| 60 ± 2* | 97 ± 1 |
Xanomeline
| 65 ± 5* | 69 ± 7* |
AC-42
| 63 ± 3* | 69 ± 1* |
AC-260584
| 59 ± 2* | 64 ± 3* |
- HEK-293 cells expressing hM1 were treated with various ligands for 30 minutes as indicated in the table. Concentrations of ligands used were as follows; carbachol, 100 μM; oxotremorine-M, 1 μM; xanomeline, 100 μM; AC-42, 10 μM; and AC-260584, 1 μM and similar to concentration used in the internalization assays. Values presented are % receptors on the cells surface. Data presented is the average from 2 independent experiments carried out in triplicate. Statistically significant difference compared to no drug, * = p < 0.05, (Student t-test, GraphPad, Prism).
- No recycling could be observed after treatment with NDMC (1 μM), 71% cell surface receptor after 3 hours of recycling (n = 1).