Selectivity of bradykinin analogues for receptors mediating contraction and relaxation of the rat duodenum.

ABSTRACT

1. Bradykinin produces a biphasic response in the rat duodenum that consists of a relaxation (pD2 = 8.44) followed by a contraction (pD2 = 6.91). 2. The B1 agonist des-Arg9-bradykinin produced a contraction (pD2 = 7.16) but no relaxation. Des-Arg9-[Leu8]-bradykinin, which is a B1 antagonist in other systems produced contraction (pD2 = 7.65) in the rat duodenum. 3. Four bradykinin analogues that are preferential B2 agonists in other tissues had a biphasic effect with pD2 values in the range 7.22-8.68 for relaxation and 6.26-6.91 for contraction. 4. [Thi5,8,D-Phe7]-bradykinin, which is a B2 antagonist in most other systems produced relaxation in the rat duodenum, with a pD2 of 7.49. 5. It is concluded that the contractile component of the response to bradykinin in rat duodenum may be mediated by a subtype of the B1 receptor and the relaxant component by a receptor of the B2 subtype.