Characterization of [3H]MEN 11420, a novel glycosylated peptide antagonist radioligand of the tachykinin NK2 receptor

Biochem Biophys Res Commun. 1998 Jul 9;248(1):78-82. doi: 10.1006/bbrc.1998.8883.

Abstract

[3H]MEN 11420, a radiolabeled glycosylated peptide antagonist of the tachykinin NK2 receptor, has been investigated in ligand-receptor binding assays using membranes of CHO cells transfected with the human tachykinin NK2 receptor. [3H]MEN 11420 bound to a single class of high affinity binding sites: its binding was inhibited by natural tachykinins (potency ranking: NKA >> SP > or = NKB), as well as by peptide (MEN 11420 > MEN 10376 >> R 396) and nonpeptide (SR 48968 > GR 159897) selective NK2 receptor antagonists. These data indicate that [3H]MEN 11420 is a potent radioligand for the human tachykinin NK2 receptor that may represent a useful tool for studying ligand-receptor interactions at the molecular level.

MeSH terms

  • Animals
  • Binding Sites
  • Binding, Competitive
  • CHO Cells
  • Cricetinae
  • Humans
  • Kinetics
  • Peptides, Cyclic / metabolism*
  • Radioligand Assay
  • Receptors, Neurokinin-2 / antagonists & inhibitors*
  • Receptors, Neurokinin-2 / genetics
  • Receptors, Neurokinin-2 / metabolism
  • Tachykinins / metabolism
  • Tachykinins / pharmacology
  • Transfection

Substances

  • MEN 11420
  • Peptides, Cyclic
  • Receptors, Neurokinin-2
  • Tachykinins