Abstract
The melanocortin-1 receptor (MC-1R) is a G-protein-coupled receptor involved in inflammation and skin pigmentation. Compound 2 is the first highly potent and selective MC-1R small-molecule agonist reported. Compound 2 showed efficacy in an acute model of inflammation, which has demonstrated the role of MC-1R in modulation of inflammation.
MeSH terms
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Acute Disease
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis*
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology
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Combinatorial Chemistry Techniques
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Humans
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Inflammation / chemically induced
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Inflammation / metabolism
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Lipopolysaccharides
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Mice
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Mice, Inbred BALB C
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Receptors, Corticotropin / agonists*
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Receptors, Melanocortin
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Structure-Activity Relationship
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Tumor Cells, Cultured
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Tumor Necrosis Factor-alpha / antagonists & inhibitors
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Tumor Necrosis Factor-alpha / biosynthesis
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Tyrosine / analogs & derivatives*
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Tyrosine / chemical synthesis*
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Tyrosine / pharmacology
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Lipopolysaccharides
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Receptors, Corticotropin
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Receptors, Melanocortin
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Tumor Necrosis Factor-alpha
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Tyrosine