Glibenclamide is a competitive antagonist of the thromboxane A2 receptor in dog coronary artery in vitro

1 Glibenclamide, a sulphonylurea oral hypoglycaemic agent is a widely used antagonist of cromakalim‐activated K+ channels in smooth muscle. 2 In isolated ring segments of the large circumflex coronary artery from the dog, glibenclamide (1–30 μm) caused a concentration‐dependent reduction in both spo...

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Bibliographic Details
Published in:British journal of pharmacology 1990-06, Vol.100 (2), p.375-378
Main Authors: Cocks, Thomas M., King, Susannah J., Angus, James A.
Format: Article
Language:English
Subjects:
15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid
Animals
Coronary Vessels - drug effects
Coronary Vessels - metabolism
Dogs
Endothelins
Endothelium, Vascular - drug effects
Endothelium, Vascular - physiology
Female
Glyburide - pharmacology
In Vitro Techniques
Isometric Contraction
Male
Muscle Contraction - drug effects
Muscle, Smooth, Vascular - drug effects
Muscle, Smooth, Vascular - metabolism
Norepinephrine - pharmacology
Peptides - pharmacology
Potassium Chloride - pharmacology
Prostaglandin Endoperoxides, Synthetic - antagonists & inhibitors
Prostaglandin Endoperoxides, Synthetic - pharmacology
Receptors, Prostaglandin - antagonists & inhibitors
Receptors, Thromboxane
Thromboxane A2 - metabolism
Tolbutamide - pharmacology
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Summary:1 Glibenclamide, a sulphonylurea oral hypoglycaemic agent is a widely used antagonist of cromakalim‐activated K+ channels in smooth muscle. 2 In isolated ring segments of the large circumflex coronary artery from the dog, glibenclamide (1–30 μm) caused a concentration‐dependent reduction in both spontaneous isometric force and contractions induced by U46619, a thromboxane A2‐mimetic. 3 Glibenclamide behaved as a competitive antagonist of U46619 with an estimated pKB (‐log KB) value of 6.2 by Schild regression analysis (slope 1.07). 4 Glibenclamide (30 μm) was apparently selective since it had no effect on the concentration‐contraction curves to endothelin‐1, noradrenaline or KCl. 5 We suggest that this additional property of glibenclamide should be considered in any smooth muscle study where active force is raised by either the exogenous application or endogenous generation of thromboxane A2.
ISSN:0007-1188
1476-5381
DOI:10.1111/j.1476-5381.1990.tb15812.x