Structure−Activity Relationship of (1-Aryl-2-piperazinylethyl)piperazines: Antagonists for the AGRP/Melanocortin Receptor Binding

Agouti-related protein (AGRP) is an endogenous antagonist of the melanocortin action. 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...

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Veröffentlicht in:	Journal of medicinal chemistry 2003-01, Vol.46 (1), p.9-11
Hauptverfasser:	Arasasingham, Premilla N, Fotsch, Christopher, Ouyang, Xiaohu, Norman, Mark H, Kelly, Michael G, Stark, Kevin L, Karbon, Bill, Hale, Clarence, Baumgartner, James W, Zambrano, Martha, Cheetham, Janet, Tamayo, Nuria A
Format:	Artikel
Sprache:	eng
Schlagworte:	Agouti-Related Protein alpha-MSH - antagonists & inhibitors alpha-MSH - metabolism Binding Sites Biological and medical sciences Hormones. Endocrine system Humans Intercellular Signaling Peptides and Proteins Medical sciences Pharmacology. Drug treatments Piperazines - chemical synthesis Piperazines - chemistry Piperazines - pharmacology Proteins - antagonists & inhibitors Proteins - metabolism Receptor, Melanocortin, Type 4 Receptors, Corticotropin - antagonists & inhibitors Receptors, Corticotropin - metabolism Structure-Activity Relationship
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Zusammenfassung:	Agouti-related protein (AGRP) is an endogenous antagonist of the melanocortin action. 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.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm0255522