Design, synthesis, and biological activities of a potent and selective alpha-melanotropin antagonist.

@article{AlObeidi1990DesignSA,
  title={Design, synthesis, and biological activities of a potent and selective alpha-melanotropin antagonist.},
  author={Fahad A Al-Obeidi and Victor J. Hruby and Mac E. Hadley and Tomi Kim Sawyer and Ana Maria de Lauro Castrucci},
  journal={International journal of peptide and protein research},
  year={1990},
  volume={35 3},
  pages={
          228-34
        }
}
Based on structure-activity relationships of the potent alpha-MSH agonist, Ac-Nle4-Asp5-His6-D-Phe7-Arg8-Trp9-Lys10-NH2, several analogs of the general formula Ac-Nle4-Asp5-Waa6-Xaa7-Yaa8-Zaa9-Lys10+ ++-NH2 were synthesized and tested on frog and lizard skin bioassays for their possible inhibitory actions against alpha-MSH on melanocyte stimulation. When Waa6 = Trp, Xaa7 = D-Phe, Yaa8 = Nle and Zaa = Trp, a highly potent alpha-MSH antagonist, Ac-Nle-Asp-Trp-D-Phe-Nle-Trp-Lys-NH2, with… CONTINUE READING