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British Journal of Pharmacology logoLink to British Journal of Pharmacology
. 1987 Dec;92(4):851–855. doi: 10.1111/j.1476-5381.1987.tb11390.x

New synthetic antagonists of bradykinin.

M Schachter 1, Y Uchida 1, D J Longridge 1, T Labedz 1, E T Whalley 1, R J Vavrek 1, J M Stewart 1
PMCID: PMC1853719  PMID: 3427282

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.

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Selected References

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