SR 142801, the first potent non-peptide antagonist of the tachykinin NK3 receptor

Life Sci. 1995;56(1):PL27-32. doi: 10.1016/0024-3205(94)00413-m.


SR 142801 is the first potent and selective non-peptide antagonist of the tachykinin NK3 receptor. It inhibited [MePhe7]NKB binding to its receptor from various species, including humans. SR 142801 was a competitive antagonist of [MePhe7]NKB-mediated contractions of guinea-pig ileum and inhibited the acetylcholine release following the activation of the guinea-pig ileum tachykinin NK3 receptor. In vivo, SR 142801 potently inhibited the turning behaviour induced by intrastriatal injection of senktide in gerbils, and appears as a powerful tool for investigation of the physiological and pathological role of NKB and its NK3 receptor.

MeSH terms

  • Animals
  • Behavior, Animal / drug effects
  • Dose-Response Relationship, Drug
  • Gerbillinae
  • Guinea Pigs
  • In Vitro Techniques
  • Neurokinin B / analogs & derivatives
  • Neurokinin B / antagonists & inhibitors
  • Neurokinin B / metabolism
  • Piperidines / pharmacology*
  • Rats
  • Receptors, Neurokinin-3 / antagonists & inhibitors*
  • Vasoconstriction / drug effects


  • Piperidines
  • Receptors, Neurokinin-3
  • neurokinin B, MePhe(7)-
  • Neurokinin B
  • SR 142801