TABLE 1

MC1R Affinities of α-MSH Analogs

α-MSH analogIC50 (nmol/L) *
α-MSH1.65 ± 0.18
NAPamide0.27 ± 0.07 †
DOTA-NAPamide1.19 ± 0.19
I0.59 ± 0.16 †
II2.86 ± 0.34 †
III13.75 ± 1.86 †
IV2.13 ± 0.29 †
V4.23 ± 0.58 †
VI46.12 ± 13.5 †
VII8.73 ± 1.63 †

  • ↵* MC1R affinity of α-MSH analogs was assessed by competition binding experiments with B16F1 cells and 125I-NDP-MSH as radioligand (mean ± SEM; n = 3–16).

  • ↵† P < 0.05 vs. DOTA-NAPamide.