Labat C, Cerrina J, Raffestin B, Brink C
INSERM U200, Université Paris Sud, Clamart, France.
Respiration. 1989;55(4):220-6. doi: 10.1159/000195738.
In human bronchial muscle preparations contracted with histamine, the rank order potency for the relaxant effect of various antagonists was: thiazinamium chloride less than tripelennamine less than atropine (pD2 values: 7.78, 6.16 and greater than 4 for each antagonist, respectively). These antagonists also relaxed human isolated bronchial muscle preparations contracted with acetylcholine. The rank order potency was: atropine less than thiazinamium chloride less than tripelennamine (pD2 values: 7.76, 6.94 and 4.05, respectively). Tripelennamine and thiazinamium chloride displaced histamine concentration-effect curves and atropine and thiazinamium chloride antagonized acetylcholine curves in human isolated bronchial muscle preparations. These results suggest that thiazinamium chloride may have important therapeutic value in airways disease since this drug not only relaxed human isolated airway muscle preparations but also antagonized contractile responses in these tissues to both histamine and acetylcholine.
在与组胺收缩的人支气管肌肉制剂中,各种拮抗剂的松弛作用效价顺序为:氯化噻嗪铵<曲吡那敏<阿托品(pD2值:每种拮抗剂分别为7.78、6.16和大于4)。这些拮抗剂也能松弛与乙酰胆碱收缩的人离体支气管肌肉制剂。效价顺序为:阿托品<氯化噻嗪铵<曲吡那敏(pD2值:分别为7.76、6.94和4.05)。在人离体支气管肌肉制剂中,曲吡那敏和氯化噻嗪铵使组胺浓度 - 效应曲线移位,阿托品和氯化噻嗪铵拮抗乙酰胆碱曲线。这些结果表明,氯化噻嗪铵在气道疾病中可能具有重要的治疗价值,因为这种药物不仅能松弛人离体气道肌肉制剂,还能拮抗这些组织对组胺和乙酰胆碱的收缩反应。