Jones T, Denis D, Hall R, Ethier D
Prostaglandins. 1983 Nov;26(5):833-43. doi: 10.1016/0090-6980(83)90066-7.
Leukotrienes D4 greater than C4 greater than E4 greater than F4 produced qualitatively similar contractions of guinea-pig trachealis, which were antagonized by the SRS-antagonist FPL-55712. Schild analyses indicated that FPL-55712 when tested in a low concentration range (0.57 - 5.7 X 10(-6) M) was a competitive antagonist of LTC4, LTE4 and LTF4 (slope not significantly different from one). The interaction of FPL-55712 with LTD4 may be noncompetitive (slope less than 1). Comparison of the calculated dissociation constants (-log KB) indicated that FPL-55712 was more effective at blocking LTE4 and LTF4 compared to LTC4 and LTD4. In the presence of higher concentrations of FPL-55712 (1.9 X 10(-5) M) the antagonism of LTC4 became noncompetitive. These findings indicate that important differences exist in the interaction of FPL-55712 with the various peptido leukotrienes in guinea pig trachealis. Discovery of more selective antagonists will be needed to determine if multiple receptor subtypes are present in this tissue.
白三烯D4、C4、E4和F4对豚鼠气管产生性质相似的收缩作用，这些收缩作用可被SRS拮抗剂FPL - 55712拮抗。希尔分析表明，当在低浓度范围（0.57 - 5.7×10⁻⁶ M）进行测试时，FPL - 55712是LTC4、LTE4和LTF4的竞争性拮抗剂（斜率与1无显著差异）。FPL - 55712与LTD4的相互作用可能是非竞争性的（斜率小于1）。计算得出的解离常数（-log KB）比较表明，与LTC4和LTD4相比，FPL - 55712在阻断LTE4和LTF4方面更有效。在较高浓度的FPL - 55712（1.9×10⁻⁵ M）存在时，LTC4的拮抗作用变为非竞争性。这些发现表明，FPL - 55712与豚鼠气管中各种肽白三烯的相互作用存在重要差异。需要发现更具选择性的拮抗剂来确定该组织中是否存在多种受体亚型。
