LONG-ACTING, ORALLY-ACTIVE BRADYKININ ANTAGONISTS FOR A WIDE-RANGE OFAPPLICATIONS

Actions of bradykinin (Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg; BK) are me diated 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 pathophys iological 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.