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曲氟柳的一种代谢物2-羟基-4-三氟甲基苯甲酸与其他药物之间的体外蛋白质结合相互作用。

In-vitro protein binding interaction between a metabolite of triflusal, 2-hydroxy-4-trifluoromethylbenzoic acid and other drugs.

作者信息

Mis R, Ramis J, Conte L, Forn J

机构信息

Research Centre, J. Uriach & Co., Barcelona, Spain.

出版信息

J Pharm Pharmacol. 1992 Nov;44(11):935-7. doi: 10.1111/j.2042-7158.1992.tb03241.x.

Abstract

2-Hydroxy-4-trifluoromethylbenzoic acid (HTB) is the main active metabolite of triflusal, an antiplatelet drug. The in-vitro binding of HTB to human serum was studied in the presence of different drugs. The results indicate that no statistically significant changes are observed in the HTB binding in the presence of caffeine, theophylline, glisentide, enalapril, cimetidine or warfarin. The free fraction of HTB increases significantly in the presence of the non-steroidal anti-inflammatory drugs studied: diclofenac, ibuprofen, indomethacin, naproxen, piroxicam and salicylic acid. At high concentrations, HTB displaces these anti-inflammatory drugs and also glisentide and warfarin from their protein binding sites.

摘要

2-羟基-4-三氟甲基苯甲酸(HTB)是抗血小板药物曲氟柳的主要活性代谢产物。在不同药物存在的情况下,研究了HTB与人血清的体外结合情况。结果表明,在咖啡因、茶碱、格列齐特、依那普利、西咪替丁或华法林存在时,HTB的结合未观察到统计学上的显著变化。在所研究的非甾体抗炎药(双氯芬酸、布洛芬、吲哚美辛、萘普生、吡罗昔康和水杨酸)存在时,HTB的游离分数显著增加。在高浓度时,HTB会将这些抗炎药以及格列齐特和华法林从它们的蛋白质结合位点上置换下来。

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