MCH potencies at the wild-type and mutant MCHR1 receptors
Mutants with complete loss of function are in bold. Data represent the mean ± S.E.M. of at least three independent experiments.
| Variant | MCH-Induced Gαq5i/SRE5x Luciferase Activity | MCH-Mediated Inhibition of Forskolin-Induced CRE6x-Luciferase Activity | ||||
|---|---|---|---|---|---|---|
| MCH EC50 | pEC50 ± S.E.M. | Significance vs. WT | MCH EC50 | pEC50 ± S.E.M. | Significance vs. WT | |
| nM | nM | |||||
| MCHR1 WT | 103 | 6.99 ± 0.06 | 5.9 | 8.23 ± 0.14 | ||
| T25M | 85 | 7.07 ± 0.11 | N.S. | 3.3 | 8.48 ± 0.17 | N.S. |
| D28V | 65 | 7.19 ± 0.22 | N.S. | 5.0 | 8.30 ± 0.12 | N.S. |
| D32N | 76 | 7.12 ± 0.19 | N.S. | 6.6 | 8.18 ± 0.21 | N.S. |
| G34R | 79 | 7.10 ± 0.14 | N.S. | 5.7 | 8.18 ± 0.33 | N.S. |
| G103R | 142 | 6.85 ± 0.20 | N.S. | 9.6 | 8.02 ± 0.23 | N.S. |
| Y107H | 351 | 6.46 ± 0.12 | ** | 20.0 | 7.70 ± 0.29 | N.S. |
| R210H | N.D. | N.D. | N.D. | N.D. | N.D. | N.D. |
| Y250H | 91 | 7.04 ± 0.18 | N.S. | 6.2 | 8.21 ± 0.27 | N.S. |
| T305M | 173 | 6.76 ± 0.11 | N.S. | 19.5 | 7.71 ± 0.34 | N.S. |
| P377S | N.D. | N.D. | N.D. | N.D. | N.D. | N.D. |
| G401R | 49 | 7.31 ± 0.16 | N.S. | 2.7 | 8.57 ± 0.49 | N.S. |
| T411M | 109 | 6.96 ± 0.17 | N.S. | 2.8 | 8.56 ± 0.60 | N.S. |
N.S., not significant; N.D., not determined.
↵** P < 0.01.