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体外给予17β-雌二醇可抑制药物诱导的大鼠离体精囊收缩。

In vitro administration of 17 beta-estradiol inhibits drug-induced contractions of the rat isolated seminal vesicle.

作者信息

Chandranath S I

机构信息

Department of Pharmacology, Faculty of Medicine & Health Sciences, U.A.E. University, Al Ain, United Arab Emirates.

出版信息

Gen Pharmacol. 1997 Oct;29(4):681-6. doi: 10.1016/s0306-3623(96)00564-2.

Abstract
  1. The rat isolated seminal vesicle responded to noradrenaline (NA), acetylcholine (ACh), potassium chloride (KCl) and barium chloride (BaCl2) with reproducible contractions. 2. 17 beta-estradiol (17 beta E) cumulatively added in the isolated organ bath reduced the number of contractions with all agonists used in the rank order of potency: BaCl2 > or = KCl > ACh > NA. The dose-response curves constructed in the presence of 17 beta E (2 x 10(-5) mol/l) produced a rightward shift and a reduction in the maximum response showing inhibitory activity. 3. When the calcium content in the normal Krebs medium (2.5 mmol/l) was reduced to half, the inhibitory activity of 17 beta E was potentiated. The maximum inhibition rates to KCl (phasic and tonic), BaCl2 and ACh were significantly (P < 0.05) different from each other. 4. The inhibitory effects of 17 beta E against all agonists tested were found to be similar in their responses to verapamil, but were much lower in potency. 5. The inhibitory effects of 17 beta E was seen only when the hormone was present in the tissue environment and was readily reversible as soon as the tissue was washed with the Krebs medium, suggesting that the effect of 17 beta E is localized. 6. It is suggested that the in vitro application of 17 beta E on the rat isolated seminal vesicle interferes with the process of translocation of calcium ions from the extracellular medium.
摘要
  1. 大鼠离体精囊对去甲肾上腺素(NA)、乙酰胆碱(ACh)、氯化钾(KCl)和氯化钡(BaCl₂)产生可重复的收缩反应。2. 在离体器官浴中累积添加17β-雌二醇(17βE)可减少所有激动剂引起的收缩次数,其效力顺序为:BaCl₂≥KCl>ACh>NA。在存在17βE(2×10⁻⁵mol/L)的情况下构建的剂量-反应曲线出现右移且最大反应降低,显示出抑制活性。3. 当正常 Krebs 培养基中的钙含量(2.5mmol/L)减半时,17βE 的抑制活性增强。对 KCl(相性和紧张性)、BaCl₂和 ACh 的最大抑制率彼此之间存在显著差异(P<0.05)。4. 发现17βE 对所有测试激动剂的抑制作用在对维拉帕米的反应方面相似,但效力要低得多。5. 仅当组织环境中存在该激素时才可见17βE 的抑制作用,并且一旦用 Krebs 培养基冲洗组织,该作用即可迅速逆转,这表明17βE 的作用是局部性的。6. 提示在体外将17βE 应用于大鼠离体精囊会干扰钙离子从细胞外介质的转运过程。

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