Related Experiment Video
Updated: Aug 10, 2026

A Method to Study the C924T Polymorphism of the Thromboxane A2 Receptor Gene
Published on: April 1, 2019
Interspecies differences in thromboxane A2 receptors are distinguished by glibenclamide
1Department of Pharmacology, Monash University, Clayton, Victoria, Australia.
Abstract:
The ability of the thromboxane A2 receptor antagonist, GR32191 ([1R-[1alpha(Z),2beta3beta,5alpha]]-7-[5-[[(1,1'-biphe nyl)-4-yl]methoxy]-3-hydroxy-2-(1-piperidinyl)cyclopentyl]-4-heptenoic acid), and the sulphonylurea, glibenclamide, to antagonise contractions to the thromboxane A2 mimetic, U46619 ((15S)-hydroxy-11alpha,9alpha(epoxymethano)prosta-5Z, 13E-dienoic acid), were assessed in rat and guinea-pig isolated large (aorta) and small (mesentery and coronary) arteries. U46619 concentration-response curves were constructed in the absence and presence of GR32191 and glibenclamide and pKB values calculated. GR32191 caused significant rightward shifts in U46619 concentration-response curves and was a more potent antagonist in guinea-pig vessels (pKB approximately 9.4) than rat arteries (pKB approximately 7.9). Conversely, glibenclamide failed to inhibit contractions to U46619 in guinea-pig vessels but antagonised responses to U46619 in rat aorta (pKB = 6.1) and mesenteric artery (pKB = 6.3). In combination, GR32191 and glibenclamide caused a shift in the concentration-effect curve to U46619 in rat aorta that was additive. These results suggest that glibenclamide can discriminate between species differences in thromboxane A2 receptors and may exert its inhibitory effect upon U46619-mediated contractions at the level of the thromboxane A2 receptor.
More Related Videos
Related Concept Videos
Adrenergic Receptors: ɑ Subtype
Adrenaline ≥ Noradrenaline >> Isoprenaline
α-adrenoceptors are further divided into α1 and α2-adrenoceptors.
α1-Adrenoceptors: These receptors are located postsynaptically on the effector organs and cause constriction of smooth muscle mediated by activation of phospholipase C—inositol-1,4,5-trisphosphate...
Adrenergic Antagonists: ɑ and β-Receptor Blockers
Pharmacogenetic Phenotypes: Alterations in Pharmacokinetics, Drug Targets and Biologic Milieu
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase
Oral Hypoglycemic Agents: Glinides
Dipeptidyl Peptidase 4 Inhibitors

