Bhattacherjee P, Eakins K E
Br J Pharmacol. 1974 Feb;50(2):227-30. doi: 10.1111/j.1476-5381.1974.tb08565.x.
1 We have compared the sensitivity of the prostaglandin synthetase systems derived from microsomal fractions of rabbit ocular tissues (anterior uvea, conjunctiva and retina) with other rabbit tissues such as the kidney medulla and spleen, to inhibition by indomethacin.2 Generation of prostaglandin-like activity by the microsomal fractions from added arachidonic acid varied with the tissue used. Highest activity was found in the kidney medulla, then in descending order, the conjunctiva, anterior uvea, spleen, retina and cornea.3 Indomethacin was most potent in the spleen (ID(50) 0.045 mug/ml) then in decreasing order in the kidney medulla, conjunctiva, anterior uvea and weakest in the retina, where the ID(50) for indomethacin was 50 mug/ml.4 The differential sensitivity to inhibition of the prostaglandin synthetase systems from different tissues is an important consideration in the development of new ocular anti-inflammatory agents.
我们已将源自兔眼组织(前葡萄膜、结膜和视网膜)微粒体部分的前列腺素合成酶系统与其他兔组织(如肾髓质和脾脏)对吲哚美辛抑制作用的敏感性进行了比较。
从添加的花生四烯酸中由微粒体部分产生的类前列腺素活性随所用组织而变化。在肾髓质中发现活性最高,然后依次为结膜、前葡萄膜、脾脏、视网膜和角膜。
吲哚美辛在脾脏中效力最强(半数抑制浓度为0.045微克/毫升),然后在肾髓质、结膜、前葡萄膜中效力依次降低,在视网膜中最弱,吲哚美辛在视网膜中的半数抑制浓度为50微克/毫升。
不同组织的前列腺素合成酶系统对抑制作用的差异敏感性是开发新型眼部抗炎药物时的一个重要考虑因素。