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Nonapeptide-1 is an antagonist of melanocortin receptor 1 (MC1R; Ki = 40 nM in COS-1 cells expressing human receptors).1 It is selective for MC1R over MC3R, MC4R, and MC5R (Kis = 470, 1,340, and 2,400 nM, respectively). Nonapeptide-1 inhibits cAMP accumulation and melanosome dispersion induced by α-melanocyte-stimulating hormone (α-MSH) in melanocytes with IC50 values of 2.5 and 11 nM, respectively.2
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1. Characterization of the binding of MSH-
2. Discovery and structure-