Table 2.
Sample of Melanocortin Receptor Binding Agents Studied with Erection
| Structure | Preferential MCR Binding (3 vs. 4) |
MC3R affinity Ki (nM)* |
MC4R affinity Ki (nM)* |
|
|---|---|---|---|---|
| Agonists | ||||
| ACTH | 39 amino acid peptide SYSMEHFRWGKPVGKKRRPVKVYP DAGEDQSAEAFPLEF |
3,4 | ||
| α-MSH | Ac-Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly-Lys-Pro-Val-NH2 | 3,4 | 30 | 5 |
| MT-II | Ac-Nle-c (Asp-His-D-Phe-Arg-Trp-Lys)-NH2 | 3,4 | 1.3 | 1.1 |
| PT-141 | Ac-Nle-c (Asp-His-D-Phe-Arg-Trp-Lys)-OH | 3,4 | N/A | N/A |
| PB-III-93 | H-Tyr-Val-Met-Gly-His-Phe-Arg-D-Trp-Asp-Arg-Phe-Gly-OH | 3 | 6.7 | 600 |
| THIQ | N-[(3R)-1,2,3,4-tetrahydroisoquinolinium-3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol-1-ylmethyl)piperidin-1-yl]-2-oxoethylamine |
4 | 761 | 1.2 |
| Antagonists | ||||
| AgRP | 132 amino acid peptide | 3,4 | 4.5 | 3.5 |
| SHU-9119 | Ac-Nle-c[Asp-His-D-Nal(2′)-Arg-Trp-Lys]-NH2 | 3,4 | 0.23 | 0.06 |
| MPB 10 | c(6β→10ε)[succinyl6-D-(2′)Nal7-Arg8-Trp9-Lys10]-NH2 | 4 | 150 | 0.5 |
| AVM-127 | c[Nle-Val-D-Nal(2′)-Arg-Trp-Glu]-NH2 | 3 | 1.7 | 180 |
| HS-014 | Ac-c[Cys-Glu-His-D-Nal(2′)-Arg-Trp-Gly-Cys]-Pro-Pro-Lys-Asp-NH2 | 4 | 54.4 | 3.16 |