New synthetic antagonists of bradykinin

Br J Pharmacol. 1987 Dec;92(4):851-5. doi: 10.1111/j.1476-5381.1987.tb11390.x.

Abstract

1 A new synthetic bradykinin analogue was found to be an antagonist of bradykinin-induced vascular permeability in rabbit skin. It was effective in equimolar concentrations. 2 These analogues also antagonized the action of bradykinin in contracting the guinea-pig isolated ileum. The mean pA2 values of five different antagonists ranged from 5.3-6.4 respectively, on this preparation. 3 Our observations, together with those of others suggest that these antagonists act on the same receptor types, viz., B2, in rabbit blood vessels and in smooth muscle of guinea-pig ileum. 4 Our results support the view that the way is now promising for the synthesis of potent specific antagonists of bradykinin for experimental and therapeutic use.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Bradykinin / antagonists & inhibitors*
  • Capillary Permeability / drug effects
  • Guinea Pigs
  • Histamine / pharmacology
  • In Vitro Techniques
  • Male
  • Muscle, Smooth / drug effects*
  • Rabbits
  • Regional Blood Flow / drug effects
  • Skin / drug effects

Substances

  • Histamine
  • Bradykinin