Ahnfelt-Rønne I, Arrigoni-Martelli E
Agents Actions Suppl. 1979(4):110-9.
A radiochemical method is described which allows simultaneous determination of the in vitro effects of chemical substances on thromboxane and prostacyclin synthesis. The method utilizes the capacity of a combination of bovine seminal vesicle microsomes (BSVM) and rabbit lung microsomes (TbLM) to transform arachidonic acid into TXB2, 12-hydroxy-heptadecatrienoic acid (HHT), 6-keto-PGF1 alpha (6K-PGF1 alpha), PGF2 alpha, and PGE2 in the ratio of 1:0.80:0.63:0.13:0.05, respectively. Imidazole and burimamide, and to some degree also dipyridamole and L8027, were found to be selective thromboxane inhibitors. The preferential alternative pathways following thromboxane inhibition with these drugs were towards PGE2 and PGF2 alpha, and the algebraic sum of arachidonic acid metabolism was not affected by imidazole and burimamide. The assay is a convenient method for identification of drugs which interfere with specific pathways of arachidonic acid metabolism.
本文描述了一种放射化学方法，该方法可同时测定化学物质对血栓素和前列环素合成的体外效应。该方法利用牛精囊微粒体（BSVM）和兔肺微粒体（TbLM）的组合能力，将花生四烯酸分别以1:0.80:0.63:0.13:0.05的比例转化为TXB2、12-羟基-十七碳三烯酸（HHT）、6-酮-PGF1α（6K-PGF1α）、PGF2α和PGE2。发现咪唑和布立马胺，以及在一定程度上双嘧达莫和L8027是选择性血栓素抑制剂。用这些药物抑制血栓素后，优先的替代途径是生成PGE2和PGF2α，咪唑和布立马胺不影响花生四烯酸代谢的代数和。该测定法是鉴定干扰花生四烯酸代谢特定途径的药物的便捷方法。
