New synthetic antagonists of bradykinin.
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.
Schachter
M
M
Department of Physiology, University of Alberta, Edmonton, Canada.
Uchida
Y
Y
Longridge
D J
DJ
Labedz
T
T
Whalley
E T
ET
Vavrek
R J
RJ
Stewart
J M
JM
D000818:Animals; D001920:Bradykinin / Q000037:antagonists & inhibitors*; D002199:Capillary Permeability / Q000187:drug effects; D006168:Guinea Pigs; D006632:Histamine / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D009130:Muscle, Smooth / Q000187:drug effects*; D011817:Rabbits; D012039:Regional Blood Flow / Q000187:drug effects; D012867:Skin / Q000187:drug effects
D006632:Histamine; D001920:Bradykinin