Development of an efficient and selective radioligand for bradykinin B1 receptor occupancy studies

Bioorg Med Chem Lett. 2004 Dec 20;14(24):6045-8. doi: 10.1016/j.bmcl.2004.09.074.

Abstract

We have developed an efficient and selective radioligand, the [35S]-radiolabeled dihydroquinoxalinone derivative, 4, for an ex vivo receptor occupancy assay in transgenic rats over-expressing the human bradykinin B1 receptor.

MeSH terms

  • Animals
  • Animals, Genetically Modified
  • Binding, Competitive / drug effects
  • Bradykinin B1 Receptor Antagonists*
  • Humans
  • Isotope Labeling
  • Ligands
  • Quinoxalines / chemical synthesis*
  • Quinoxalines / pharmacology*
  • Radioligand Assay
  • Rats
  • Receptor, Bradykinin B1 / chemistry
  • Structure-Activity Relationship
  • Sulfur Radioisotopes

Substances

  • Bradykinin B1 Receptor Antagonists
  • Ligands
  • Quinoxalines
  • Receptor, Bradykinin B1
  • Sulfur Radioisotopes