BINDING OF INDOMETHACIN TO HUMAN-SERUM ALBUMIN - ITS NON DISPLACEMENT BY VARIOUS AGENTS, INFLUENCE OF FREE FATTY-ACIDS AND THE UNEXPECTED EFFECT OF INDOMETHACIN ON WARFARIN-BINDING

被引：72

作者：

ZINI, R ^{[1
]}

DATHIS, P ^{[1
]}

BARRE, J ^{[1
]}

TILLEMENT, JP ^{[1
]}

机构：

[1] HOP BOCAGE,DEPT INFORMAT MED,F-21034 DIJON,FRANCE

来源：

BIOCHEMICAL PHARMACOLOGY | 1979年 / 28卷 / 17期

关键词：

D O I：

10.1016/0006-2952(79)90043-1

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Binding of indomethacin to HSA was studied in vitro by equilibrium dialysis. Our results show that binding to HSA is 97 per cent at therapeutic levels. Binding is characterized by several saturable numbers of binding sites (n = 8) with a moderate association constant (K= 1.2. 104M-1) and by another nonsaturable phenomenon (nK = 4200 M-1). Furthermore, acetylsalicylic acid (ASA), salicylic acid (SA), 1 anilinonaphtalene-8-sulfonic acid (ANS), chlorophenoxyisobutyrate (CPIB), digitoxin, tryptophan and warfarin do not alter indomethacin binding. On the other hand, free fatty acids (FFA) decrease indomethacin binding in human serum albumin (HSA). Moreover indomethacin markedly decreases warfarin binding. © 1979.

引用

页码：2661 / 2665

页数：5

共 24 条

[1]

ASHBROOK JD, 1975, J BIOL CHEM, V250, P2333

[2] FATTY-ACID CONTENT AND DRUG BINDING CHARACTERISTICS OF COMMERCIAL ALBUMIN PREPARATIONS [J].