Matzner Y, Drexler R, Levy M
Eur J Clin Invest. 1984 Dec;14(6):440-3. doi: 10.1111/j.1365-2362.1984.tb01210.x.
Dipyrone metabolites 4-methylaminoantipyrine (MAA) and 4-formylaminoantipyrine (FAA) as well as acetylsalicylic acid inhibited neutrophil migration toward zymosan-activated serum. Inhibition was maximal (76.8 +/- 19.0; 79.2 +/- 12.5 and 80.0 +/- 4.4%, respectively, P less than 0.003) when suboptimal concentrations (0.3%) of the chemoattractant were used and could be demonstrated with drug concentrations comparable with plasma concentrations obtained in clinical use. Acetaminophen and other dipyrone metabolites 4-aminoantipyrine (AA) and 4-acetylaminoantipyrine (AAA) lacked chemotactic inhibitory potential. Only MAA and FAA inhibited mildly neutrophil random migration (18.1 +/- 7.8 and 11.2 +/- 3.4%, respectively). We suggest that blocking neutrophil movement plays a role in the anti-inflammatory activity of dipyrone and acetylsalicylic acid, but their mechanism of inhibition remains obscure.
安乃近代谢产物4-甲基氨基安替比林(MAA)和4-甲酰氨基安替比林(FAA)以及乙酰水杨酸可抑制中性粒细胞向酵母聚糖激活血清的迁移。当使用次优浓度(0.3%)的趋化因子时,抑制作用最大(分别为76.8±19.0;79.2±12.5和80.0±4.4%,P<0.003),并且在与临床使用中获得的血浆浓度相当的药物浓度下即可表现出来。对乙酰氨基酚以及安乃近的其他代谢产物4-氨基安替比林(AA)和4-乙酰氨基安替比林(AAA)缺乏趋化抑制潜能。只有MAA和FAA轻度抑制中性粒细胞随机迁移(分别为18.1±7.8和11.2±3.4%)。我们认为,阻断中性粒细胞运动在安乃近和乙酰水杨酸的抗炎活性中起作用,但其抑制机制仍不清楚。