POTENT BLOCK OF CL- CHANNELS BY ANTIALLERGIC DRUGS

被引：29
作者：
REINSPRECHT, M
PECHT, I
SCHINDLER, H
ROMANIN, C
机构：
[1] UNIV LINZ,INST BIOPHYS,A-4040 LINZ,AUSTRIA
[2] WEIZMANN INST SCI,DEPT CHEM IMMUNOL,IL-76100 REHOVOT,ISRAEL
来源：
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1992年 / 188卷 / 03期
关键词：
D O I：
10.1016/0006-291X(92)91325-K
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Two antiallergic drugs, cromolyn and RU 31156, were examined for their potency to block intermediate-conductance Cl- channels. For this, single Cl- channel activities of mucosal-type mast cells (RBL-2H3) and alternatively, of colonic carcinoma cells (HT29) were monitored employing the patch-clamp technique in the inside-out patch configuration. Here we show that intermediate-conductance Cl- channels of either cell type were blocked by both compounds. Cl- channel inhibition occurred by a slow rather than a flickering block and with a Hill coefficient around 1. RU 31156 was about one order of magnitude more potent (IC50 about 1 μM) than cromolyn. The (IC50 values of each compound were not significantly different (p < 0.01) in the two cell types. Our data provide evidence for two novel Cl- channel blockers, which may be of further use in Cl- channel characterization as well as purification. © 1992.
引用
收藏
页码：957 / 963
页数：7
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