[3H]NMS binding parameters in wild-type and mutant M2 and M5 receptors
Data represent mean values ± S.E. of three or more independent experiments or mean values of two independent experiments along with the single values, respectively.
| Dissociation t1/2 | k-1 | pKD ([3H]NMS) | |
|---|---|---|---|
| min | min-1 | ||
| M2 wild type | 6.8 ± 0.2 | 0.1031 ± 0.0027 | 10.13 ± 0.06 |
| M2422W→A | 13.0 ± 0.4 | 0.0504 ± 0.0025 | 9.61 ± 0.07 |
| M2423T→A | 8.5 ± 0.3 | 0.0823 ± 0.0029 | 9.89 (9.88; 9.91) |
| M2423T→H | 22.9 ± 0.9 | 0.0316 ± 0.0012 | 9.90 ± 0.08 |
| M2427W→A | 35.9 ± 1.3 | 0.0192 ± 0.0001 | 9.88 ± 0.16 |
| M2177Y→Q + 422W→A | 5.6 ± 0.1 | 0.1253 ± 0.0018 | 9.62 (9.56; 9.67) |
| M2422W→A + 423T→H | 45.0 ± 1.1 | 0.0155 ± 0.0004 | 9.82 (9.76; 9.87) |
| M2422W→A + 427W→A | 56.4 ± 1.5 | 0.0126 ± 0.0003 | 9.86 ± 0.06 |
| M5 wild type | 121.7 ± 3.4 | 0.0058 ± 0.0002 | 9.91 ± 0.08 |
| M5477W→A | 110.9 ± 4.8 | 0.0061 ± 0.0002 | 9.97 (9.98; 9.96) |
| M5478H→A | 63.8 ± 0.6 | 0.0109 ± 0.0001 | 9.77 (9.80; 9.74) |
| M5478H→T | 41.7 ± 1.6 | 0.0167 ± 0.0007 | 9.89 (9.92; 9.86) |
| M5482W→A | 83.6 ± 2.2 | 0.0084 ± 0.0003 | 9.92 ± 0.08 |
| M5477W→A + 478H→T | 50.8 ± 2.6 | 0.0142 ± 0.0008 | 9.91 (9.93; 9.89) |
| M5477W→A + 482W→A | 117.1 ± 7.7 | 0.0056 ± 0.0002 | 9.62 ± 0.06 |
Dissociation t1/2, half time of dissociation of [3H]NMS in the absence of allosteric modulator; k-1, rate constant of [3H]NMS dissociation; pKD, minus log value of the equilibrium dissociation constant of [3H]NMS binding.