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目的 :研究选择性磷酸二酯酶 (phosphodies terase ,PDE)Ⅳ抑制剂Ariflo对内皮素 1(endothelin 1,ET 1)诱发的非妊娠人子宫平滑肌收缩的影响。方法 :累积给药法观察药物对离体平滑肌收缩的作用。结果 :Ariflo可降低子宫平滑肌自主收缩的收缩频率及收缩幅度 (pD2 =7.90 ) ,且对ET 1(3×10 -8mol·L-1)诱发的子宫平滑肌收缩具有浓度依赖性抑制作用 (pD2 =7.4 0 ) ,作用强度与Rolipram相似。结论 :Ariflo对ET 1诱发的离体人子宫平滑肌的收缩具有显著抑制作用 ,提示在临床上有缓解痛经的作用。
OBJECTIVE: To study the effects of Ariflo, a selective phosphodiesterase (PDE) inhibitor Ⅳ, on the contraction of non-pregnant uterine smooth muscle induced by endothelin 1 (ET 1). Methods: Cumulative drug administration was used to observe the effect of drugs on isolated smooth muscle contraction. Results: Ariflo could reduce the contractile frequency and contraction amplitude of uterine smooth muscle spontaneous contraction (pD2 = 7.90) and inhibit the uterine smooth muscle contraction induced by ET 1 (3 × 10 -8 mol·L-1) in a dose-dependent manner (pD2 = 7.4 0), similar to Rolipram. CONCLUSION: Ariflo has a significant inhibitory effect on the contractile activity of isolated human uterine smooth muscle induced by ET 1, suggesting a clinically useful role in alleviating dysmenorrhea.