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新型磷酸二酯酶Ⅳ抑制剂Ariflo对内皮素-1诱发离体人子宫平滑肌收缩的影响 被引量:1

Effects of a novel phosphodiesterase IV inhibitor Ariflo on endothelin-1-induced contractility of isolated human uterine myometrium
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摘要 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。 AIM: To investigate the effects of selective phosphodiesterase (PDE) IV inhibitor Ariflo on the contractility of nonpregnant human uterine myometrium induced by endothelin 1 (ET 1). METHODS: Contractile responses to Ariflo were accumulated in isolated human myometrium. RESULTS: Ariflo could inhibit both the frequency and amplitude of autonomic contraction of myometrium (pD 2 = 7.90 ) and ET 1 induced contraction in a concentration dependent manner (pD 2= 7.40 ), with a potency similar to that of Rolipram. CONCLUSION: Ariflo has the effect of inhibition on endothelin 1 induced contractility of the isolated human uterine myometrium evidently.
出处 《中国临床药理学与治疗学》 CAS CSCD 2004年第3期299-301,共3页 Chinese Journal of Clinical Pharmacology and Therapeutics
基金 中法INSERM SSMU合作项目 (№ 2 0 0 2 10 )
关键词 磷酸二酯酶Ⅳ抑制剂 内皮素-1 子宫平滑肌 痛经 洛利普兰 phosphodiesterase IV inhibitor endothelin 1 uterine myometrium dysmenorrhea rolipram
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  • 1Stephen A B,J Urol,1998年,159卷,2164页

共引文献17

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  • 1孙超渊,张莉,程克棣,杜冠华,朱平.磷酸二酯酶4研究进展[J].中国药理学通报,2006,22(10):1161-1167. 被引量:19
  • 2Richard F J, Regulation of meiotic maturation [J]. J Anim Sci,2007, 85(13 Suppl) :E4-6.
  • 3Palmer M J, Bell AS, Fox DN, et al. Design of second generation phosphodiesterase5inhibitors[J]. Curr Top Med Chem,2007,7(4) :405- 419.
  • 4Omori K, Kotera J. Overview of PDEs and their regulation [ J ]. Circ Res. 2007,100 ( 3 ) : 309 -327.

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