Potent, long-acting, orally-active bradykinin antagonists for a wide range of applications

Abstract Actions of bradykinin (Arg–Pro–Pro–Gly–Phe–Ser–Pro–Phe–Arg; BK) are mediated by constitutively expressed B2 receptors, that require the full BK peptide chain, and by B1 receptors, induced in inflammation, that use BK(1–8) as ligand. In addition to many physiological and pathophysiological functions, the growth factor activity of BK evidently allows it to act as an autocrine stimulant for small cell lung cancer. A new group of BK antagonists containing the novel amino acid a-(2-indanyl)glycine provides extremely potent broad-spectrum as well as selective antagonists for all these functions.