Parks W M, Hoak J C, Czervionke R L
J Pharmacol Exp Ther. 1981 Nov;219(2):415-9.
Ibuprofen (Motrin) decreases infarct size in animal models of myocardial infarction. Inasmuch as this effect might be related to the inhibitory effect of ibuprofen on platelet function, we have evaluated its effect on platelet and endothelial prostaglandin synthesis. Human umbilical vein endothelial cultures and washed human platelets were studied. Thromboxane (TX)A2 was determined by radioimmunoassay for its stable and product TXB2 and prostacyclin was determined by radioimmunoassay for its stable end product 6-keto-prostaglandin F1 alpha. At all concentrations of ibuprofen tested, platelet TXA2 and endothelial prostacyclin synthesis were inhibited to a similar degree. Unlike aspirin, the effect of ibuprofen on prostaglandin synthesis was rapidly reversible in both endothelial and platelet systems after removal of the drug. Ibuprofen was also shown to interfere with the irreversible inhibitory effect of aspirin, suggesting that ibuprofen and aspirin might compete for binding by the cyclooxygenase. Inhibition of endothelial and platelet prostaglandin synthesis was nearly complete with 100 microM concentrations of aspirin (100%) and ibuprofen (99%). Thrombin-stimulated platelet adherence to endothelial monolayers was related inversely to the amount of prostacyclin produced by the endothelium. Adherence was maximal at concentrations (100 microM) of ibuprofen and aspirin producing near complete inhibition of prostaglandin synthesis. Maximal adherence with both drugs was comparable (28 vs. 31%). Ibuprofen showed no preferential inhibitory effect on TXA2 synthesis and, at a 100 microM concentration, was as effective as aspirin in the systems studied.
布洛芬（Motrin）可减小心肌梗死动物模型中的梗死面积。鉴于此效应可能与布洛芬对血小板功能的抑制作用有关，我们评估了其对血小板和内皮前列腺素合成的影响。我们研究了人脐静脉内皮细胞培养物和洗涤后的人血小板。通过放射免疫分析法测定血栓素（TX）A2的稳定产物TXB2来确定血栓素A2，通过放射免疫分析法测定前列环素的稳定终产物6-酮-前列腺素F1α来确定前列环素。在所有测试的布洛芬浓度下，血小板TXA2和内皮前列环素的合成受到相似程度的抑制。与阿司匹林不同，在去除药物后，布洛芬对前列腺素合成的影响在内皮和血小板系统中均可迅速逆转。布洛芬还被证明会干扰阿司匹林的不可逆抑制作用，这表明布洛芬和阿司匹林可能竞争环氧合酶的结合位点。当阿司匹林（100%）和布洛芬（99%）的浓度达到100微摩尔时，对内皮和血小板前列腺素合成的抑制几乎完全。凝血酶刺激的血小板与内皮单层的黏附与内皮产生的前列环素量呈负相关。在布洛芬和阿司匹林浓度为100微摩尔时，黏附达到最大值，此时前列腺素合成几乎完全被抑制。两种药物的最大黏附率相当（28%对31%）。布洛芬对TXA2合成没有优先抑制作用，在100微摩尔浓度下，在所研究的系统中与阿司匹林效果相同。
