Table 3.
Reported Ki values (nM) for muscarinic ligands in cell lines expressing human muscarinic receptor subtypes
| Compound | M1 | M2 | M3 | M4 | M5 |
|---|---|---|---|---|---|
| Trospiuma | 0.8 | 0.6 | 0.5 | 1.0 | 1.9 |
| Atropine | 0.3 | 0.8–1.3 | 0.2–0.3 | 0.1–1.2 | 0.2–0.8 |
| AQ-RA 741 | 29–62 | 3.7–4.4 | 55–86 | 1.5–15 | 732–831 |
| 4-DAMP | 0.6–1.2 | 4–9 | 0.4–1.0 | 0.7–1.7 | 0.6–1.3 |
| Methoctramine | 41–112 | 13–20 | 214–954 | 32–78 | 134–398 |
| Darifenacin | 7–35 | 44–77 | 0.8–1.3 | 18–46 | 5–9 |
| AF-DX 116 | 417–740 | 64–73 | 786–1290 | 211–545 | 5130 |
| Pirenzepine | 6–9 | 224–407 | 75–184 | 17–48 | 66–158 |
Values in bold indicate preferred receptor subtype.
Data from references cited in Mansfield et al. (2003).
a
Data from Madersbacher (2003).