钾通道开放剂的抗过敏作用及其机制  

THE ANTIANAPHYLACTIC ACTION OF POTASSIUM CHANNEL OPENERS AND ITS MECHANISM

作　　者：王佩[1,2] 徐建华[1,2] 魏尔清 

机构地区：[1]浙江医科大学药学系药理教研室 [2]浙江医科大学基础医学院

出　　处：《药学学报》1997年第12期888-892,共5页Acta Pharmaceutica Sinica

摘　　要：用多种抗变态反应实验方法，研究钾通道开放剂米诺地尔（Ｍｉｎ）与二氮嗪（Ｄｉａ）的抗过敏作用，并探讨其作用机制。结果表明，Ｍｉｎ能抑制大鼠同种被动皮肤过敏反应，拮抗５ＨＴ引起的大鼠皮肤血管通透性增高。Ｄｉａ和Ｍｉｎ均能抑制豚鼠离体回肠平滑肌的过敏性收缩，Ｄｉａ并能抑制Ａ２３１８７和化合物４８／８０诱发的肥大细胞释放组胺。因此钾通道开放剂Ｍｉｎ与Ｄｉａ具有抗过敏作用，作用的主要机理是抑制肥大细胞外Ｃａ２＋内流和细胞内贮存钙的释放，从而抑制组胺的释放。The antianaphylactic action of potassium channel openers was studied and reported in this paper. Minoxidil(Min) was shown to inhibit passive cutaneous anaphylaxis in rats. Diazoxide(Dia) and Min were found to inhibit antigeninduced guineapig ileum smooth muscle contraction in vitro. Min was shown to antagonize 5HTinduced capillary permeability in rat skin. Dia was demonstrated to inhibit histamine release from rat peritoneal mast cells induced by A23187 and compound 48/80, but it failed to antagonize guineapig ileum smooth muscle contraction induced by histamine in vitro. These results provide evidence that potassium channel openers may be a new group of inhibitors of histamine release and indicate that the mechanism of its antianaphylactic action may be related to its potassium channel opening effect. As a result of this effect, Ca2+ influx to the mast cells decreases and Ca2+ release from calcium storage was inhibited, thus inhibting histamine release.

关 键 词：钾通道开放剂 米诺地尔 二氮嗪 抗过敏 肥大细胞 组胺释放 

分 类 号：R976[医药卫生—药品]