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Potent, long-acting, orally-active bradykinin antagonists for a wide range of applications
J M Stewart1, L Gera, D C Chan
1Department of Biochemistry, University of Colorado Medical School, Denver 80262, USA. john.stewart@uchsc.edu
Immunopharmacology
|June 1, 1997
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.