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本文介绍一种快速简便,待测药品需用量小的前列腺素合成酶抑制剂类抗炎药的离体筛选方法。将牛精囊腺微粒体与花生四烯酸等共同温育20分钟,培液中合成的PGE_2水平经放射兔疫分析可达10μg/L;萘普生可明显抑制该法中PGE_2的合成,培液中PGE_2的水平与药物浓度呈负相关线性关系。将此法用于系列新型化合物的筛选,发现其中若干化合物具有明显的抑制PGE_2合成作用。
This article describes a quick and easy, the required test drugs need a small amount of prostaglandin synthase inhibitor anti-inflammatory drugs in vitro screening method. The bovine serum albumin microsome and arachidonic acid and other incubated for 20 minutes, the PGE 2 level in the culture fluid by radioactive vaccine analysis up to 10μg / L; naproxen can significantly inhibit the synthesis of PGE 2, The level of PGE_2 in liquid was negatively correlated with drug concentration. This method was applied to the screening of a series of new compounds and found that some of them had significant inhibitory effect on the synthesis of PGE_2.