Synthesis and biological evaluation in vitro of selective, high affinity peptide antagonists of human melanin-concentrating hormone action at human melanin-concentrating hormone receptor 1.

@article{Bednarek2002SynthesisAB,
  title={Synthesis and biological evaluation in vitro of selective, high affinity peptide antagonists of human melanin-concentrating hormone action at human melanin-concentrating hormone receptor 1.},
  author={Maria A. Bednarek and Donna L. Hreniuk and Carina P. Tan and Oksana C. Palyha and Douglas J. Macneil and Lex H. T. van der Ploeg and Andrew D. Howard and Scott D. Feighner},
  journal={Biochemistry},
  year={2002},
  volume={41 20},
  pages={
          6383-90
        }
}
Human melanin-concentrating hormone (hMCH) and many of its analogues are potent but nonspecific ligands for human melanin-concentrating hormone receptors 1 and 2 (hMCH-1R and hMCH-2R). To differentiate between the physiological functions of these receptors, selective antagonists are needed. In this study, analogues of Ac-Arg(6)-cyclo(S-S)(Cys(7)-Met(8)-Leu(9)-Gly(10)-Arg(11)-Val(12)-Tyr(13)-Arg(14)-Pro(15)-Cys(16))-NH(2), a high affinity but nonselective agonist at hMCH-1R and hMCH-2R, were… Expand
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S36057 is a more potent and more stable radioligand than [125I]‐[3‐iodo Tyr13]‐MCH that will represent a reliable tool for binding assays in the search of novel MCH ligands and should provide great help for autoradiographic studies of the MCH receptor distribution in the central nervous system. Expand
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