Table 3.
Receptor expression (% of WT) |
125I- ACTH binding Ki (nM) |
cAMP production EC50 (nM) |
|
---|---|---|---|
hMC2RWT | 100 | 8.6 ± 1.0 | 4.8 ± 0.1 |
N81A | 89 ± 12.4 | 15.9 ± 0.6* | 11.6 ± 1.2* |
D104N | 78 ± 13.4 | 87.3 ± 9.8* | 87.7 ± 9.3* |
F108A | 65 ± 10.2 | >103* | >103* |
T164A | 93 ± 14.2 | 6.4 ± 0.7 | 3.9 ± 0.1 |
F168A | 56 ± 9.5 | 217.8 ± 13* | 327.6 ± 30.3* |
F244A | 95 ± 11.2 | 9.9 ± 0.9 | 4.9 ± 0.9 |
P<0.05 compared with WT receptor