Ligand binding properties of Y403F mutant and wild-type m2 muscarinic receptor
| K | Δ(ΔG°) (kcal · mol−1) | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Y403F | Wild-type | Kb | |||||||
| Antagonist | pm | pm | |||||||
| [3H]NMS | 630 ± 240 (5) | 253 ± 45 (15) | 0.54 ± 0.22 | ||||||
| [3H]QNB | 29.3 ± 3.4 (3) | 17.4 ± 2.8 (16) | 0.31 ± 0.10 | ||||||
| K H | K M | α1-a | K H | K M | K L | α1-a | K H b | K M b | |
| Agonist | nm | μm | nm | μm | μm | ||||
| Acetylcholine | 107 ± 51 (3) | 101 ± 36 (4) | 950 ± 560 | 1.45 ± 0.49 (12) | 0.350 ± 0.087 (15) | 11.1 ± 3.9 (13) | 240 ± 100 | 2.55 ± 0.25 | 3.36 ± 0.21 |
| Carbachol | 390 ± 170 (5) | 248 ± 68 (5) | 630 ± 320 | 3.6 ± 0.80 (19) | 1.37 ± 0.16 (38) | 21.7 ± 3.7 (37) | 380 ± 100 | 2.77 ± 0.26 | 3.08 ± 0.16 |
| Oxotremorine M | 51 ± 43 (5) | 25.8 ± 4.5 (5) | 500 ± 430 | 2.16 ± 0.89 (10) | 0.40 ± 0.14 (16) | 13.0 ± 8.2 (9) | 190 ± 100 | 1.88 ± 0.49 | 2.47 ± 0.22 |
| Pilocarpine | 2370 ± 680 (6) | 149 ± 52 (7) | 63 ± 29 | 27 ± 17 (8) | 2.78 ± 0.73 (14) | 25 ± 16 (9) | 100 ± 70 | 2.65 ± 0.39 | 2.36 ± 0.24 |
Values are the weighted mean ± 95% confidence interval; the number of experimental determinations are indicated in parentheses.
Δ(ΔG°) values are presented ± 95% confidence interval.
↵1-a α is calculated as the quotient of the parameters K M and K H.
1-b Equilibrium constant for which the Δ(ΔG°) values are calculated.