Bradykinin analogues: differential agonist and antagonist activities suggesting multiple receptors

Abstract

Bradykinin analogues with specific antagonist activity in several bioassays were evaluated for effects on [³H]-bradykinin receptor binding sites and inositol phosphate production in neuroblastoma N1E-115 cells. The analogues varied in their affinities for bradykinin receptors in guinea-pig ileum and N1E-115 cell membranes, in their effects on uterine and ileal contractions and in their agonist or antagonist activity on phosphoinositide turnover in N1E-115 cells. These tissue specific effects suggest the presence of multiple bradykinin receptor subtypes.