α‐Melanocyte‐stimulating hormone structure‐activity studies: Comparative analysis of melanotropic and CNS bioactivities

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Abstract
The structure-activity relationships in vitro of α-MSH (α-melanocyte-stimulating hormone, α-melanotropin) analogs as determined on normal and transformed (melanoma cell) melanocyte bioassays are summarized. Specifically, the characterization of potent and metabolically stable melanotropic agonist analogs and a newly discovered antagonist of α-MSH are highlighted. Comparison of these data versus the known structure-activity relationships of α-MSH related to CNS bioactivities suggests the existence of nonclassical α-MSH receptor-mediated pathways or, perhaps, a yet undefined endogenous neuropeptidergic pathway(s) having different selectivities for α-MSH analogs. In summary, several of the α-MSH analogs reported here may be useful molecular probes in future strategies aimed at the identification and systematic characterization of both peripheral and central α-MSH receptors.