New synthetic antagonists of bradykinin.

M Schachter, Y Uchida, DJ Longridge… - British journal of …, 1987 - ncbi.nlm.nih.gov
M Schachter, Y Uchida, DJ Longridge, T Labedz, ET Whalley, RJ Vavrek, JM Stewart
British journal of pharmacology, 1987ncbi.nlm.nih.gov
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 …
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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