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目的:探讨新型抗变态反应药N-对氟苄基-3-[(N-4-吡啶)-乙酸胺]-吲哚-45(acetamide-45)对组胺和乙酰甲胆碱引起的豚鼠离体气管收缩的影响.方法:以acetamide-45预处理气管标本后,以累积剂量法给予组胺和乙酰甲胆碱,观察acetamide-45对组胺和乙酰甲胆碱量效曲线的影响.气管张力的变化通过换能器转变为电信号并由记录仪记录.结果:Acetamide-45(1-30μmol/L)浓度依赖地抑制组胺和乙酰甲胆碱引起的豚鼠离体气管收缩.Acetamide-45(3,10,30μmol/L)使组胺的量效曲线的最大效应下降了21％—51％,使组胺的EC_(50)值(95％可信限)分别增加到31.1(24.4—39.8),34.7(26.8-45.0)和134.4(82.2-220.0)μmol/L.另一方面,acetamide-45更有效地抑制乙酰甲胆碱引起的豚鼠离体气管收缩.结论:Acetamide-45抑制由组胶和乙酰甲胆碱引起的豚鼠离体气管收缩,提示acetamide-45的抑制作用是非特异性地作用于组胺受体或胆碱能受体.
OBJECTIVE: To investigate the effect of a novel anti-allergic agent, N-p-fluorobenzyl-3 - [(N-4-pyridyl) -acetamide-45] on the histamine and methacholine-induced guinea pigs To investigate the effect of acetamide-45 on the histamine and methacholine dose-response curves.Methods: After pretreatment of trachea with acetamide-45, histamine and methacholine were administered by cumulative dose. The change of tracheal tension was converted to electrical signal by transducer and recorded by recorder.RESULTS Acetamide-45 (1-30 μmol / L) inhibited concentration-dependently the histamine and methacholine induced tracheal contraction in guinea pigs.Acetamide -45 (3, 10, 30μmol / L) decreased the maximum effect of histamine dose-response curve by 21% -51%, and increased the histamine EC50 value (95% confidence limit) to 31.1 24.4-39.8), 34.7 (26.8-45.0) and 134.4 (82.2-220.0) μmol / L. On the other hand, acetamide-45 inhibited methacholine-induced tracheal contraction more effectively in guinea pigs.Conclusion: Acetamide-45 Inhibition of tracheal contraction of guinea pig trachea induced by both micelles and methacholine suggests that the inhibitory effect of acetamide-45 acts nonspecifically on histamine receptors or cholinergic receptors.