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.
Department of Physiology, University of Alberta, Edmonton, Canada.
M
M
Schachter
Y
Y
Uchida
D J
DJ
Longridge
T
T
Labedz
E T
ET
Whalley
R J
RJ
Vavrek
J M
JM
Stewart
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