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  • Title: Alpha-melanocyte-stimulating hormone structure-activity studies: comparative analysis of melanotropic and CNS bioactivities.
    Author: Sawyer TK, Hadley ME, Hruby VJ, Castrucci AM, Staples DJ, Farah J, O'Donohue TL.
    Journal: Synapse; 1988; 2(3):289-92. PubMed ID: 2850630.
    Abstract:
    The structure-activity relationships in vitro of alpha-MSH (alpha-melanocyte-stimulating hormone, alpha-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 alpha-MSH are highlighted. Comparison of these data versus the known structure-activity relationships of alpha-MSH related to CNS bioactivities suggests the existence of nonclassical alpha-MSH receptor-mediated pathways or, perhaps, a yet undefined endogenous neuropeptidergic pathway(s) having different selectivities for alpha-MSH analogs. In summary, several of the alpha-MSH analogs reported here may be useful molecular probes in future strategies aimed at the identification and systematic characterization of both peripheral and central alpha-MSH receptors.
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