Characterization of the prostanoid receptors mediating constriction and relaxation of human isolated uterine artery

1 This study was undertaken to characterize pharmacologically the prostanoid receptor subtypes mediating constriction and relaxation of human isolated uterine artery. 2 U‐46619 was a potent constrictor agonist on human uterine artery (EC50 [95% CL] = 3.5 [1.8‐6.7] μM). Prostaglandin E2 (PGE2α), PGF2...

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Bibliographic Details
Published in:British journal of pharmacology 1995-09, Vol.116 (1), p.1692-1696
Main Authors: Baxter, G.S., Clayton, J.K., Coleman, R.A., Marshall, K., Sangha, R., Senior, J.
Format: Article
Language:English
Subjects:
15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid
Arteries - ultrastructure
Biological and medical sciences
Biphenyl Compounds - pharmacology
Blood vessels and receptors
Epoprostenol - pharmacology
Female
Fundamental and applied biological sciences. Psychology
Heptanoic Acids - pharmacology
human uterine artery
Humans
In Vitro Techniques
IP‐receptors and relaxation
Muscle Contraction - physiology
Muscle Relaxation - physiology
Muscle, Smooth, Vascular - drug effects
Muscle, Smooth, Vascular - physiology
Muscle, Smooth, Vascular - ultrastructure
Prostaglandin Antagonists - pharmacology
Prostaglandin Endoperoxides, Synthetic - pharmacology
Prostanoid receptors
Receptors, Prostaglandin - agonists
Receptors, Prostaglandin - classification
Receptors, Prostaglandin - physiology
Thromboxane A2 - analogs & derivatives
Thromboxane A2 - pharmacology
TP‐receptors and constriction
Uterus - blood supply
Vasoconstrictor Agents - pharmacology
Vertebrates: cardiovascular system
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Summary:1 This study was undertaken to characterize pharmacologically the prostanoid receptor subtypes mediating constriction and relaxation of human isolated uterine artery. 2 U‐46619 was a potent constrictor agonist on human uterine artery (EC50 [95% CL] = 3.5 [1.8‐6.7] μM). Prostaglandin E2 (PGE2α), PGF2, PGD2 and PGI2 only weakly constricted the uterine artery, being at least 100 times less potent than U‐46619. The PGE2 and PGI2 constrictor effects may be modified by the potent dilator effects of these compounds. A number of agonists which show selectivity for FP‐, DP‐ and EP‐receptors including ICI 81008, BW 245C, sulprostone, rioprostil and butaprost, failed to cause any constriction at concentrations up to 30 μM. 3 Constrictor responses induced by all agonists tested were reduced or abolished by the TP‐receptor blocking drugs, GR 32191 and EP 092. pA2 estimates for both antagonists versus U‐46619 were 8.50, values which are consistent with their affinities at TP‐receptors. 4 In preparations pre‐constricted with phenylephrine (1 μM) both PGI2 and PGE2 were potent relaxant agonists. The selective IP‐receptor agonists, cicaprost and iloprost, also dilated human uterine artery and were approximately 10 fold more potent than PGI2. The EP2‐receptor agonists, butaprost and rioprostil and the selective DP‐agonist, BW 245C, were at least 100 fold weaker than PGI2 and PGE2 suggesting that neither DP‐ nor EP2 receptors were involved. 5 We conclude that TP‐receptors mediate constriction, whereas IP‐ and possibly EP4‐receptors mediate relaxation of human uterine artery.
ISSN:0007-1188
1476-5381
DOI:10.1111/j.1476-5381.1995.tb16393.x