Abstract
The purpose of the present study was to characterize more precisely an inhibitory, adenylate cyclase-coupled bradykinin receptor in guinea pig ileum membranes. Therefore, the effects of various well-known bradykinin B 2 receptor antagonists were examined at the level of bradykinin-induced inhibition of ileal adenylate cyclase activity and compared with both their binding affinities and their potencies to antagonize ileal contraction evoked by bradykinin. A group of three highly potent antagonists was found to be able to antagonize both bradykinin-induced adenylate cyclase inhibition and smooth muscle contraction. Several other antagonists abolished the bradykinin-induced ileal contraction but did not influence its action on adenylate cyclase. The compound [D-Na1 1, Thi 5,8, D-Phe 7]bradykinin which is known to inhibit the bradykinin-induced contraction in the rat uterus but not in the guinea pig ileum was found to be a weak but selective antagonist for the adenylate cyclase-coupled bradykinin receptor in guinea pig ileum. Altogether, in guinea pig ileum membranes the inhibitory, adenylate cyclase-coupled bradykinin B 2 receptor with pM affinity towards bradykinin exhibits a unique antagonist profile and is distinguished from the excitatory bradykinin B 2 receptor with nM affinity towards bradykinin.
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