当前位置： SCI文献检索 > EUROPEAN JOURNAL OF PHARMACOLOGY期刊下所有文献 > Guanabenz, an alpha2-selective adrenergic agonist, activates Ca2+-dependent chloride currents in cystic fibrosis human airway epithelial cells.

Guanabenz, an alpha2-selective adrenergic agonist, activates Ca2+-dependent chloride currents in cystic fibrosis human airway epithelial cells.

Abstract：

:In cystic fibrosis respiratory epithelial cells, the absence or dysfunction of the chloride channel CFTR (Cystic Fibrosis Transmembrane conductance Regulator) results in reduced chloride ion transport. In contrast, Ca2+-stimulated Cl- secretion is intact in cystic fibrosis airway epithelia. One possible target for drug discovery aiming at treating cystic fibrosis is to correct the ionic imbalance through stimulation of alternative ionic pathways that may compensate the failure of epithelial Cl- conductance. Here, using a simple high-throughput screening assay to search for Cl- channels modulators in the cystic fibrosis nasal epithelial cell line JME-CF15, the compound guanabenz (Wytensin), an alpha2-selective adrenergic agonist was found positive. Using iodide effluxes and electrophysiological recordings, we showed that guanabenz-activated (EC50=831 nM) a DIDS (4,4'-diisothiocyanatostilbene-2,2'-disulfonic acid) sensitive and Ca2+ dependent Cl- channel (CaCC). Guanabenz activated a linear Cl- channel with unitary single-channel conductance of 8 pS. Recording calcium signals in CF15 cells showed that guanabenz increased the intracellular Ca2+ concentration stimulating an influx of Ca2+. In the absence of extracellular Ca2+, the guanabenz effects on Ca2+ influx and activation of CaCC were both abolished. These data demonstrate that guanabenz activates Ca2+-dependent Cl- channels via a Ca2+ influx in human cystic fibrosis airway epithelial cells.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Norez C,Vandebrouck C,Antigny F,Dannhoffer L,Blondel M,Becq F

doi

10.1016/j.ejphar.2008.06.103

subject

Has Abstract

pub_date

2008-09-11 00:00:00

pages

33-40

issue

1-3

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(08)00715-2

journal_volume

592

pub_type

杂志文章

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