A novel screening assay of the Na+-dependent Cl-/HCO3- exchanger (NCBE) and its inhibitors

被引：4

作者：

Faber, S ^{[1
]}

Lang, HJ ^{[1
]}

Hropot, M ^{[1
]}

Scholkens, BA ^{[1
]}

Mutschler, E ^{[1
]}

机构：

[1] UNIV FRANKFURT,DEPT PHARMACOL,D-6000 FRANKFURT,GERMANY

来源：

CELLULAR PHYSIOLOGY AND BIOCHEMISTRY | 1996年 / 6卷 / 1-2期

关键词：

Na+-dependent Cl-/HCO3- exchanger; BCECF; fibroblast; DIDS; DCDPC; diphenylamine-2-carboxylic acid; Na+-dependent Cl-/HCO3- exchange blockers;

D O I：

10.1159/000154793

中图分类号：

Q2 [细胞生物学];

学科分类号：

071009 ; 090102 ;

摘要：

A mouse fibroblast L cell line defective in Na+/H+ antiport activity (LAP1) was used to develop a screening assay for the Na+-dependent Cl-/HCO3- exchanger (NCBE). Regulation of intracellular pH (pH(i)) via NCBE was studied in suspended LAP 1 cells using the pH-sensitive fluorescent dye 2',7'-bis(2-carboxyethyl)-5,6-carboxyfluorescein. Besides the well-known irreversible NCBE blocker 4,4'-diisothiocyanatostilbene-2,2'-disulfonic acid (DIDS), different compounds were tested. None of these had any higher effect than DIDS. Nevertheless, 3',5-dichlorodiphenylamine-2-carboxylic acid and the corresponding 3'-trifluoromethyl derivative were found to be approximately as potent as DIDS with IC50 values of 29.2 +/- 2.5 and 21.7 +/- 5.7 mu M.

引用

页码：39 / 49

页数：11

共 24 条

[1] PLATELET CYTOSOLIC PROTON AND FREE CALCIUM CONCENTRATIONS IN ESSENTIAL-HYPERTENSION [J].