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. Author manuscript; available in PMC: 2009 Aug 15.
Published in final edited form as: Biochem Pharmacol. 2008 Jul 9;76(4):520–530. doi: 10.1016/j.bcp.2008.05.026

Table 2.

Ligand Binding and D-Trp8-γ-Stimulated cAMP Production of WT and Mutant hMC3Rs

hMC3R n d-Trp8-γ-MSH-stimulated cAMP
 d-Trp8-γ-MSH binding
EC50 (nM) Emax (% WT) IC50 (nM)
WT 8 0.69 ± 0.15 100 6.23 ± 1.80
E73D 4 0.42 ± 0.06 130 ± 45 5.17 ± 2.41
E73Q 4 0.70 ± 0.26 87 ± 21 5.24 ± 1.78
E80D 4 0.71 ± 0.27 32 ± 5 c 2.57 ± 1.02
E80Q 3 0.84 ± 0.31 99 ± 18 2.61 ± 0.46
D154E 3 231.80 ± 75.56a 88 ± 31 106.24 ± 30.66c
D178E 3 0.50 ± 0.13 64 ± 14 3.84 ± 1.79
E221D 3 0.65 ± 0.28 135 ± 53 5.30 ± 1.79
E221Q 3 0.58 ± 0.02 215 ± 58 5.25 ± 2.45
D332Q 3 16.99 ± 4.83a 9 ± 1 c 8.24 ± 1.85
a

significantly different from WT hMC3R, p<0.05

b

significantly different from WT hMC3R, p<0.01

c

significantly different from WT hMC3R, p<0.001

The data are expressed as the mean ± SEM of three or four independent experiments. The maximal response under d-Trp8-γ-MSH stimulation was 2162 ± 338 pmol cAMP/106 cells for WT hMC3R.