Table 1 |
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|
Affinity profiles of selective and nonselective muscarinic receptor antagonists for muscarinic M2 and M3 receptors. |
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| M2* |
M3# |
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|
|
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| 4-DAMP |
7.8 |
9.0 |
[8, 11] |
| AQ-RA 741 |
8.3 |
7.5–6.6 |
[135] |
| Gallamine |
6.5 |
4.3 |
[8] |
| DAU 5884 |
6.6 |
8.7 |
[14] |
| Methoctramine |
7.5 |
6.5 |
[8] |
| Pirenzepine |
6.2 |
6.8 |
[8, 11] |
| AF-DX 116 |
7.0 |
5.6–6.3 |
[8, 11] |
| Ipratropium |
9.7† |
9.7† |
[5] |
|
|
|||
| Tiotropium |
10.7† |
11.0† |
[5] |
|
* Data represent binding affinities (pKi) for cardiac muscarinic M2 receptors # Data represent functional affinities (pA2) to methacholine-induced contraction of tracheal and bronchial preparations. † Data represent binding affinities (pKi) to cloned human muscarinic receptor subtypes. | |||
Gosens et al. Respiratory Research 2006 7:73 doi:10.1186/1465-9921-7-73 |
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