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. 1995 Feb;114(3):612–617. doi: 10.1111/j.1476-5381.1995.tb17183.x

Bradykinin B1 receptors in the rabbit urinary bladder: induction of responses, smooth muscle contraction, and phosphatidylinositol hydrolysis.

S K Butt 1, L G Dawson 1, J M Hall 1
PMCID: PMC1510028  PMID: 7735687

Abstract

1. The aim of this study was to analyse the pharmacological characteristics, and second-messenger coupling-mechanisms, of bradykinin B1 receptors in an intact tissue, the rabbit urinary bladder; and to investigate the influence of inhibition of endogenous peptidases on kinin activities. 2. In preparations of rabbit mucosa-free urinary bladder, at 90 min after mounting of the preparations, bradykinin (1 nM-10 microM) evoked contractile responses. In contrast, the B1 receptor-selective agonist [des-Arg9]-BK (10 mM-10 microM) was only weakly active at this time. Contractile responses to [des-Arg9]-BK increased with time of tissue incubation in the organ bath, reaching a maximum after 3 h, when the pD2 estimates were 6.4 +/- 0.3 for bradykinin, and 6.9 +/- 0.2 for [des-Arg9]-BK. 3. Once stabilized, responses to [des-Arg9]-BK in the bladder were competitively antagonized by the B1 receptor-selective antagonists [Leu8,des-Arg9]-BK and D-Arg-[Hyp3,Thi5,D-Tic7,Oic8,des-Arg9]-BK ([des-Arg10]-Hoe140) (pKB estimates were 6.1 +/- 0.1 and 7.1 +/- 0.1, respectively; n = 17-21), but responses were unaffected by the B2 receptor-selective antagonist D-Arg-[Hyp3,Thi5,D-Tic7,Oic8]-BK (Hoe140) (100 nM; n = 4). Contractile responses to bradykinin itself were partially, but significantly, inhibited by the B1 receptor-selective antagonist, [Leu8,des-Arg9]-BK (10 microM) (P < 0.05), or by the B2 receptor-selective antagonist Hoe140 (100 nM) (P < 0.005) alone, and were largely blocked by a combination of the two antagonists (P < 0.0001).(ABSTRACT TRUNCATED AT 250 WORDS)

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Selected References

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