Schachter M, Uchida Y, Longridge D J, Labedz T, Whalley E T, Vavrek R J, Stewart J M
Department of Physiology, University of Alberta, Edmonton, Canada.
Br J Pharmacol. 1987 Dec;92(4):851-5. doi: 10.1111/j.1476-5381.1987.tb11390.x.
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.
一种新的合成缓激肽类似物被发现是缓激肽诱导兔皮肤血管通透性的拮抗剂。它在等摩尔浓度下有效。
这些类似物也拮抗缓激肽对豚鼠离体回肠的收缩作用。在该制剂上，五种不同拮抗剂的平均pA2值分别为5.3 - 6.4。
我们的观察结果以及其他人的观察结果表明，这些拮抗剂作用于相同的受体类型，即兔血管和豚鼠回肠平滑肌中的B2受体。
我们的结果支持这样一种观点，即现在有希望合成用于实验和治疗用途的强效缓激肽特异性拮抗剂。
