β3肾上腺素能受体激动剂对离体人肺脏肺泡液体清除的作用

Chinese Journal of Clinical Pharmacology and Therapeutics(2014)

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Abstract
目的:制备离体人肺脏模型,探讨β3肾上腺素能受体激动剂CGP-12177对肺泡液体清除率(AFC)的作用及其机制.方法:以肺泡内Ev-ans蓝标记的白蛋白浓度的变化测定AFC.首先将10-4 mol/L到10-7 mol/L的CGP-12177分别灌注到离体人肺脏肺泡腔内,测定AFC的变化.然后将10-5 mol/L CGP-12177分别与α受体阻滞剂酚妥拉明、β1受体阻滞剂阿替洛尔、β2受体阻滞剂ICI-118551、β3受体阻滞剂SR59230A、钠通道阻断剂氨氯吡咪、Na+-K+-ATP酶阻断剂哇巴因混合后灌注到离体人肺脏肺泡腔内,测定AFC的变化.结果:10-7 mol/L和10-4 mol/L CGP-12177对离体人肺脏肺泡液体清除率没有影响,10-6 mol/L和10-5 mol/L的CGP-12177能够显著提高离体人肺脏肺泡液体清除率.CGP-12177增加离体人肺脏AFC的作用能够被SR59230A、氨氯吡咪和哇巴因抑制.结论:高选择性CGP-12177主要通过调节Na+-K+-ATP酶的活性提高离体人肺脏肺泡液体清除能力.
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