Abstract
Antagonists for the melanocortin receptor family were identified by analysis of the effects of four melanocortin analogues on α-MSH(α-melanocyte-stimulating hormone)-induced cAMP accumulation in 293 human embryonal kidney (HEK) cells that expressed either the rat melanocortin MC 3 receptor, the human melanocortin MC 4 receptor or the ovine melanocortin MC 5 receptor. Two peptides, [ D-Arg 8]ACTH(adrenocorticotrope hormone)-(4–10) and [Pro 8,10, Gly 9]ACTH-(4–10), antagonized the action of α-MSH on the melanocortin MC 4 and MC 5 receptors, but not the melanocortin MC 3 receptor. [Ala 6]ACTH-(4–10) inhibited the α-MSH activation of the melanocortin MC 3 and MC 5, but only weakly antagonized the activation of the melanocortin MC 4 receptor. [Phe-I 7]ACTH-(4–10) antagonized the melanocortin MC 3, MC 4 and MC 5 receptors equally well. These antagonists were also tested to block a behavioral response induced by α-MSH. α-MSH-induced excessive grooming behavior in rats was inhibited by [Phe-I 7]ACTH-(4–10), [ D-Arg 8]ACTH-(4–10) and [Pro 8,10,Gly 9]ACTH-(4–10), but not by [Ala 6]ACTH-(4–10). This suggests that α-MSH-induced excessive grooming behavior is mediated by melanocortin MC 4 receptors.
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