Abstract
Presumed pharmacophoric groups of melanocortin peptides (naphthalene, amino or guanidine, and indole moieties) were combined in mimetics molecules looking for their favorable location for activity at melanocortin (MC) receptors. Twenty-two compounds were prepared and tested. The best of these displayed micromolar affinities for the MC receptors.
MeSH terms
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Amination
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Binding, Competitive
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Cell Line
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Humans
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Indoles / chemistry
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Indoles / metabolism*
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Iodine Radioisotopes
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Models, Chemical
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Molecular Structure
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Naphthalenes / chemistry
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Naphthalenes / metabolism*
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Oxidation-Reduction
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Peptides / chemical synthesis
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Protein Binding
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Receptor, Melanocortin, Type 3
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Receptor, Melanocortin, Type 4
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Receptors, Corticotropin / agonists
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Receptors, Corticotropin / metabolism*
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Receptors, Melanocortin
Substances
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Indoles
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Iodine Radioisotopes
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Naphthalenes
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Peptides
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Receptor, Melanocortin, Type 3
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Receptor, Melanocortin, Type 4
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Receptors, Corticotropin
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Receptors, Melanocortin
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melanocortin 5 receptor
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naphthalene
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indole