Rangachari P K, Donoff B, Vavrek R J, Stewart J M
Department of Medicine, McMaster University, Hamilton, Ontario, Canada.
Regul Pept. 1990 Oct 8;30(3):221-30. doi: 10.1016/0167-0115(90)90097-g.
We have tested the ability of several B2 antagonists on the responses of the open-circuited isolated canine tracheal epithelium to the luminal addition of Bradykinin (BK), Lys-BK, and substance P (SP). All three peptides produced biphasic changes in transmural potential difference (PD), an initial decrease (dip) followed by an increase (rise). The B2 antagonists D-Arg0 [Hyp3,Thi5,8,D-Phe7]BK (B5630) reversibly inhibited both the dips and the rise with IC50 values of 2.01 x 10(-8) and 1.54 x 10(-7) M, respectively. The responses to SP were unaffected even with high concentrations of the antagonist. Other antagonists tested [D-Phe1,7,Thi5,8]BK (B4158), [D-Phe2,7]BK (B4404), and [D-Phe7,Hyp8]BK (B5092) were ineffective.
我们测试了几种B2拮抗剂对开路离体犬气管上皮对腔内添加缓激肽（BK）、赖氨酸-缓激肽（Lys-BK）和P物质（SP）的反应的影响。所有这三种肽均引起跨膜电位差（PD）的双相变化，先是初始下降（凹陷），随后上升。B2拮抗剂D-Arg0 [Hyp3,Thi5,8,D-Phe7]BK（B5630）可逆地抑制凹陷和上升，IC50值分别为2.01×10^(-8)和1.54×10^(-7) M。即使使用高浓度的拮抗剂，对SP的反应也不受影响。所测试的其他拮抗剂[D-Phe1,7,Thi5,8]BK（B4158）、[D-Phe2,7]BK（B4404）和[D-Phe7,Hyp8]BK（B5092）均无效。
