Table 1.
Name | Structure | Functional Activity (nM) mMC3R |
Binding Affinity (nM) mMC3R |
Functional Activity (nM) mMC4R |
Binding Affinity (nM) mMC4R |
---|---|---|---|---|---|
α-MSH | Ac-Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly-Lys-Pro-Val-NH2 | Agonist 0.80±0.14 |
ND | Agonist 5.40±0.62 |
ND |
NDP-MSH | Ac-Ser-Tyr-Ser-Nle-Glu-His-DPhe-Arg-Trp-Gly-Lys-Pro-Val-NH2 | Agonist 0.098±0.013 |
0.52±0.10 | Agonist 0.21±0.03 |
0.91±0.85 |
MTII | Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH2 | Agonist 0.16±0.03 |
1.85±0.35 | Agonist 0.087±0.008 |
0.50±0.13 |
SHU9119 | Ac-Nle-c[Asp-His-DNal(2’)-Arg-Trp-Lys]-NH2 | Antagonist* 0.32 |
3.2±1.1 | Antagonist 0.040 |
0.38±0.10 |
JRH887-9 | Ac-His-DPhe-Arg-Trp-NH2 | Agonist 160±9.2 |
ND | Agonist 17±2.8 |
ND |
JRH322-18 | Ac-His-(pI)DPhe-Arg-Trp-NH2 | Antagonist* 50±1.1 |
270±146 | Agonist 25±9.8 |
4.81±4.5 |
AGRP(87-132) | Antagonist 1.4 |
2.8±0.4 | Antagonist 0.41 |
3.0±0.3 |
ND indicates values not reported.
Indicates that the antagonists also possess partial agonist activity at the mMC3R. The indicated error represents the standard error of the mean.