Abstract
Agouti-related protein (AGRP) is an endogenous antagonist of the melanocortin action.(1) In the hypothalamus, melanocortin peptide agonists act as satiety-inducing factors that mediate their action through the melanocortin-4 receptor (MC4R) whereas AGRP is an opposing orexigenic agent. Novel inhibitors of the AGRP/MC4 binding based on (piperazinylethyl)piperazines were prepared, and their structure-activity relationship was established.
MeSH terms
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Agouti-Related Protein
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Binding Sites
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Humans
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Intercellular Signaling Peptides and Proteins
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Piperazines / chemical synthesis*
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Piperazines / chemistry
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Piperazines / pharmacology
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Proteins / antagonists & inhibitors*
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Proteins / metabolism
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Receptor, Melanocortin, Type 4
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Receptors, Corticotropin / antagonists & inhibitors*
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Receptors, Corticotropin / metabolism
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Structure-Activity Relationship
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alpha-MSH / antagonists & inhibitors
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alpha-MSH / metabolism
Substances
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AGRP protein, human
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Agouti-Related Protein
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Intercellular Signaling Peptides and Proteins
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Piperazines
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Proteins
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Receptor, Melanocortin, Type 4
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Receptors, Corticotropin
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alpha-MSH