氯喷西冸和依替唑仑及衍生物与人血清白蛋白结合部位的解析

陈浩威

中国药学杂志 ›› 1994, Vol. 29 ›› Issue (S1) : 15-17.

中国药学杂志 ›› 1994, Vol. 29 ›› Issue (S1) : 15-17.
药理

氯喷西冸和依替唑仑及衍生物与人血清白蛋白结合部位的解析

  • 陈浩威
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Binding of clotiazepam and etizolam and their derivatives to humanserum albumin

  • CHEN Hao-Wei
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摘要

采用平衡透析法及荧光置换法检测了氯噻西冸和依替唑仑及衍生物与人血清白蛋白结合的结合参数和结合部位。结果显示,氧噻西冸及衍生物的结合参数n1·k1和百分结合率比依替唑仑及衍生物高;表明氯噻西冸类药比依替唑仑类药物的血清蛋白结合性较高。氯噻西冸和依替唑仑及衍生物均在血清白蛋白的第二结合部位结合,药物浓度较高时,也在第一部位结合。更有意义的是,依替唑仑类衍生物NO16可增加华法林蛋白结合物的荧光强度,提示NO16有增强华法林与血清蛋白结合性的可能。

Abstract

Binding Parameters and binding sites of clotiazepam and etizolam and their deriva-tives human serum albumin(HSA)were investigated by equitibrium dialysis and competitive dis-placement experiment of fluorescance.It Was found that binding constant n1.k1 and binding per-centage of clotiazepam and its derivatives were higher than these of etizolam and its derivatives.This is meant that clotiazepams were more tended to bind with HSA than etizolams.All cloti-azepam and etizolam and their derivatives were found to bind on site Ⅱ of HSA,as well as on siteI when concentration of drugs was high enough.It was more interesting that the derivative of e-tlzolam,NO16,was found to increase the fluorescence of warfarin with HSA.It might be possiblethat binding tendency of warfarin to HSA was intensified by NO16.

关键词

药物蛋白结合 / 氯噻西冸 / 依替唑仑

Key words

drug-protein binding / clotiazepam / etizolam / derivatives

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导出引用
陈浩威. 氯喷西冸和依替唑仑及衍生物与人血清白蛋白结合部位的解析[J]. 中国药学杂志, 1994, 29(S1): 15-17
CHEN Ho-Wei. Binding of clotiazepam and etizolam and their derivatives to humanserum albumin[J]. Chinese Pharmaceutical Journal, 1994, 29(S1): 15-17

参考文献

1 Satoru W.Taiichi.Conformational effects in the interaction of phenylbutazone with albumin studied by circulardichroism.Biochem Pharmaco,1992.43(5):931. 2 Mohammad RP.Michael SY,Christopher JB.A comparisonof drug binding sites on mammalian albumins.Biochem Pharmaco.1992,44(5):873. 3 Jiunn HL,Florencia AL,Edgar HU,et al.Species-depen-dent enantioselective plasma protein binding of MK-571,Apotent leukotriene D antagonist.Drug Metab Dispos,1990,18(4):484 4 Peter JH.Roger LN·Felix B·Stereoselective interactions of ketoprofen glucuronides with human plasma protein andserum albumin.Biochem Pharmacol.1992,44(2):291.

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