GLIBENCLAMIDE BLOCKS THE RELAXANT ACTION OF PINACIDIL AND CROMAKALIM IN AIRWAY SMOOTH-MUSCLE

被引：33
作者：
NIELSENKUDSK, JE
BANG, L
BRONSGAARD, AM
机构：
[1] Institute of Pharmacology, University of Aarhus, DK-8000 Aarhus C, The Bartholin Building
来源：
EUROPEAN JOURNAL OF PHARMACOLOGY | 1990年 / 180卷 / 2-3期
关键词：
Cromakalim; Glibenclamide; K[!sup]+[!/sup] channels; Pinacidil; Smooth muscle (airway);
D O I：
10.1016/0014-2999(90)90312-T
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
Concentration-relaxation curves for pinacidil and cromakalim were obtained in isolated guinea-pig tracheas contracted by histamine. Pinacidil produced complete relaxation with an EC50 value of 2.8 μM. The antidiabetic concentration-relaxation curve for pinacidil without changing the maximal relaxant response. Cromakalim produced 85% relaxation with an EC50 value of 1.1 μM. Glibenclamide (0.1 μM) displaced the concentration-relaxation curve to the right and at higher concentrations (1-10 μM) caused nearly complete suppression of the maximal relaxant response to cromakalim. Glibenclamide not only prevented the effects of pinacidil and cromakalim but also produced a concentration-dependent and complete reversal of submaximal relaxations produced by these drugs. Glibenclamide was a selective antagonist of the relaxation of airway smooth muscle induced by pinacidil and cromakalim. Concentration-relaxation curves for theophylline, terbutaline and verapamil were unaffected by glibenclamide. © 1990.
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页码：291 / 296
页数：6
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