Structure-activity relationship of (1-aryl-2-piperazinylethyl)piperazines: antagonists for the AGRP/melanocortin receptor binding

J Med Chem. 2003 Jan 2;46(1):9-11. doi: 10.1021/jm0255522.

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

  • Agouti-Related Protein
  • Binding Sites
  • Humans
  • Intercellular Signaling Peptides and Proteins
  • 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
  • alpha-MSH / antagonists & inhibitors
  • alpha-MSH / metabolism

Substances

  • AGRP protein, human
  • Agouti-Related Protein
  • Intercellular Signaling Peptides and Proteins
  • Piperazines
  • Proteins
  • Receptor, Melanocortin, Type 4
  • Receptors, Corticotropin
  • alpha-MSH