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[利眠宁(氯氮卓)及其代谢产物在红细胞 - 血浆和红细胞 - 缓冲液系统中的结合与分布]

[Binding and distribution of chlordiazepoxide (Radepur) and its metabolites in the erythrocyte-plasma and erythrocyte-buffer systems].

作者信息

Terhaag B

出版信息

Acta Biol Med Ger. 1976;35(10):1373-8.

PMID:1020569
Abstract

The distribution and the free concentration of chlorodiazepoxide, desmethyl-chlorodiazeoxide and demoxepam in the systems erythrocyte-plasma and erythrocyte-buffer is determined. In both systems the substances are bound by erythrocytes. A constant ratio of distribution between erythyrocyte-plasma and erythrocyte-buffer, respectively, is established beyond therapeutic concentrations. The association constants (dual reciprocal plot) of these substances are of the order of 10(4)-1-M-1. They are the same for erythrocytes and plasma. The specific binding of erythrocytes is 20-35 fold less than with plasma proteins. It is concluded that the erythrocytes are a binding intravascular subcompartment for chlorodiazepoxide and its metabolites.

摘要

测定了氯氮䓬、去甲基氯氮䓬和地莫西泮在红细胞-血浆和红细胞-缓冲液系统中的分布及游离浓度。在这两个系统中,这些物质均与红细胞结合。在治疗浓度以上,分别在红细胞-血浆和红细胞-缓冲液之间建立了恒定的分布比例。这些物质的缔合常数(双倒数作图)约为10⁴ - 1 M⁻¹。红细胞和血浆的缔合常数相同。红细胞的特异性结合比血浆蛋白低20 - 35倍。得出的结论是,红细胞是氯氮䓬及其代谢产物的血管内结合亚区室。

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