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
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
相关论文
共 13 条
  • [11] IMMUNOLOGICALLY ACTIVATED CHLORIDE CHANNELS INVOLVED IN DEGRANULATION OF RAT MUCOSAL MAST-CELLS
    ROMANIN, C
    REINSPRECHT, M
    PECHT, I
    SCHINDLER, H
    [J]. EMBO JOURNAL, 1991, 10 (12) : 3603 - 3608
  • [12] SINGH AK, 1991, AM J PHYSIOL, V260, pC51
  • [13] DIFFERENT TYPES OF BLOCKERS OF THE INTERMEDIATE-CONDUCTANCE OUTWARDLY RECTIFYING CHLORIDE CHANNEL IN EPITHELIA
    TILMANN, M
    KUNZELMANN, K
    FROBE, U
    CABANTCHIK, I
    LANG, HJ
    ENGLERT, HC
    GREGER, R
    [J]. PFLUGERS ARCHIV-EUROPEAN JOURNAL OF PHYSIOLOGY, 1991, 418 (06): : 556 - 563