吲达帕胺与血清蛋白及红细胞的结合

Binding of indapamide to serum proteins and erythrocytes.

作者信息

Urien S, Riant P, Renouard A, Coulomb B, Rocher I, Tillement J P

机构信息

Laboratoire de Pharmacologie, Faculté de Médecine, Créteil, France.

出版信息

Biochem Pharmacol. 1988 Aug 1;37(15):2963-6. doi: 10.1016/0006-2952(88)90282-1.

DOI:10.1016/0006-2952(88)90282-1

PMID:3395370

Abstract

The binding of indapamide to isolated serum proteins and erythrocytes was studied in order to understand its blood distribution. In serum, indapamide was mainly bound to alpha 1-acid glycoprotein with a high affinity (K = 73.4/mM), and to albumin and lipoproteins. Indapamide was bound to erythrocytes via a saturable process with a high affinity (K = 385/mM and N = 57 microM for an hematocrit value of 0.48), and erythrocytes were the main binding component in blood (more than 80% of indapamide was associated to erythrocytes in blood). The binding to serum proteins affected indapamide distribution in blood, and alpha 1-acid glycoprotein was shown to be the more effective protein in decreasing the amount of indapamide associated to erythrocytes.

摘要

为了解吲达帕胺的血液分布情况，研究了其与分离的血清蛋白和红细胞的结合。在血清中，吲达帕胺主要以高亲和力（K = 73.4/mM）与α1-酸性糖蛋白结合，并与白蛋白和脂蛋白结合。吲达帕胺通过一个可饱和过程以高亲和力（血细胞比容值为0.48时，K = 385/mM，N = 57 microM）与红细胞结合，红细胞是血液中的主要结合成分（血液中超过80%的吲达帕胺与红细胞相关）。与血清蛋白的结合影响了吲达帕胺在血液中的分布，并且已表明α1-酸性糖蛋白是降低与红细胞相关的吲达帕胺量方面更有效的蛋白质。