Home LiteratureArticle Details
PMID: 10193765 Published · ppublish English Journal Article

Prostanoid receptors involved in the relaxation of human pulmonary vessels.

British journal of pharmacology ·Vol. 126 ·No. 4 ·1999-02-00 ·Pages 859-66

Walch L, Labat C, Gascard JP, de Montpreville V, Brink C, Norel X

Abstract

1. To characterize the prostanoid receptors on human pulmonary smooth muscle involved in vasodilatations, isolated arteries and veins were contracted with norepinephrine (10 microM) and vessels were subsequently challenged with different prostanoid-receptor agonists in the absence or presence of selective antagonists. 2. Prostaglandin D2 (PGD2) and the selective DP-receptor agonist, BW245C, induced relaxations in the contracted human pulmonary venous preparations. The pD2 values were: 6.88+/-0.11 (n=17) and 7.31+/-0.12 (n=5), respectively. The relaxant responses induced by PGD2 were reduced by the selective DP-receptor antagonist, BWA868C, and the estimated pA2 value was 7.84+/-0.16 (n=4). PGD2 and BW245C did not relax contracted human pulmonary arteries. 3. The selective IP-receptor agonists, iloprost and cicaprost, both induced relaxations in the contracted human vascular preparations. The pD2 values for iloprost were: 7.84+/-0.08 (n=6) and 8.25+/-0.06 (n=4) and for cicaprost: 8.06+/-0.12 (n=5) and 8.11+/-0.09 (n=5) in arteries and veins respectively. 4. Prostaglandin E2 (PGE2) and the EP2/EP3-receptor agonist, misoprostol, partially relaxed the contracted venous preparations and the pD2 values were: 8.10+/-0.15 (n=15) and 6.24+/-0.33 (n=3), respectively. These relaxations suggest the presence of an EP receptor in the human pulmonary veins. The contracted human pulmonary arteries did not relax when challenged with PGE2. 5. In human pulmonary venous preparations, the PGE2-induced relaxations were neither modified by treatment with TP/EP4-receptor antagonist, AH23848B (10 and 30 microM, n=6), nor by the DP/EP1/EP2-receptor antagonist, AH6809 (3 microM, n=6). 6. These data suggest that the relaxation induced by prostanoids involved DP-, IP-receptors and to a lesser extent an EP-receptor on human pulmonary venous smooth muscle. In contrast, only the IP-receptor is involved in the prostanoid induced relaxations on human pulmonary arterial smooth muscle.

MeSH Terms
Female Humans Hydantoins/pharmacology Iloprost/pharmacology In Vitro Techniques Male Middle Aged Norepinephrine/pharmacology Prostaglandin D2/pharmacology Prostaglandins E/pharmacology Pulmonary Artery/physiology Pulmonary Veins/physiology Receptors, Prostaglandin/physiology Vasodilation/drug effects
Chemicals
Hydantoins Prostaglandins E Receptors, Prostaglandin BW 245C Iloprost Prostaglandin D2 Norepinephrine
Authors & Affiliations
6 authors, click to expand affiliations / ORCID
Walch L
CNRS ERS 566, Centre Chirurgical Marie Lannelongue, Le Plessis-Robinson, France.
Labat C
Gascard J P
de Montpreville V
Brink C
Norel X
References (38)
38 references, click to expand
  1. Cloning and expression of the EP2 subtype of human receptors for prostaglandin E2.
    Biochem Biophys Res Commun. 1993 Nov 30;197(1):263-70 PMID: 8250933
  2. Prostaglandin receptors coupled to adenylyl cyclase in the iris-ciliary body of rabbits, cats and cows.
    Exp Eye Res. 1993 Mar;56(3):327-33 PMID: 8386102
  3. Cloning and expression of a cDNA for the human prostanoid IP receptor.
    J Biol Chem. 1994 Apr 22;269(16):12173-8 PMID: 7512962
  4. Endothelium dependence of prostanoid-induced relaxation in human hand veins.
    Acta Physiol Scand. 1994 Mar;150(3):267-72 PMID: 8010134
  5. A novel inhibitory prostanoid receptor in piglet saphenous vein.
    Prostaglandins. 1994 Feb;47(2):151-68 PMID: 8016385
  6. Characterization of the prostaglandin E2 sensitive (EP)-receptor in the rat isolated trachea.
    Br J Pharmacol. 1994 May;112(1):133-6 PMID: 8032634
  7. Cloning of a novel human prostaglandin receptor with characteristics of the pharmacologically defined EP2 subtype.
    Mol Pharmacol. 1994 Aug;46(2):213-20 PMID: 8078484
  8. Molecular cloning of human prostacyclin receptor cDNA and its gene expression in the cardiovascular system.
    Circulation. 1994 Oct;90(4):1643-7 PMID: 7923647
  9. International Union of Pharmacology classification of prostanoid receptors: properties, distribution, and structure of the receptors and their subtypes.
    Pharmacol Rev. 1994 Jun;46(2):205-29 PMID: 7938166
  10. Potent contractile actions of prostanoid EP3-receptor agonists on human isolated pulmonary artery.
    Br J Pharmacol. 1994 Oct;113(2):369-74 PMID: 7834185
  11. Characterization of prostanoid receptors on rat neutrophils.
    Br J Pharmacol. 1994 Oct;113(2):581-7 PMID: 7834211
  12. Molecular cloning and characterization of the human prostanoid DP receptor.
    J Biol Chem. 1995 Aug 11;270(32):18910-6 PMID: 7642548
  13. Comparison of the EP receptor subtypes mediating relaxation of the rabbit jugular and pig saphenous veins.
    Prostaglandins. 1995 Apr;49(4):225-37 PMID: 7667504
  14. 6-Isopropoxy-9-oxoxanthene-2-carboxylic acid (AH 6809), a human EP2 receptor antagonist.
    Biochem Pharmacol. 1995 Nov 9;50(10):1731-3 PMID: 7503778
  15. Interaction of BW A868C, a prostanoid DP-receptor antagonist, with two receptor subtypes in the rabbit isolated saphenous vein.
    Prostaglandins. 1996 Aug;52(2):125-39 PMID: 8880898
  16. Relaxant actions of nonprostanoid prostacyclin mimetics on human pulmonary artery.
    J Cardiovasc Pharmacol. 1997 Apr;29(4):525-35 PMID: 9156364
  17. Characterization of the prostanoid receptor(s) on human blood monocytes at which prostaglandin E2 inhibits lipopolysaccharide-induced tumour necrosis factor-alpha generation.
    Br J Pharmacol. 1997 Sep;122(1):149-57 PMID: 9298541
  18. Prostanoid receptors involved in the relaxation of human bronchial preparations.
    Br J Pharmacol. 1999 Feb;126(4):867-72 PMID: 10193766
  19. Some quantitative uses of drug antagonists.
    Br J Pharmacol Chemother. 1959 Mar;14(1):48-58 PMID: 13651579
  20. Molecular mechanisms of diverse actions of prostanoid receptors.
    Biochim Biophys Acta. 1995 Oct 26;1259(1):109-19 PMID: 7492609
  21. The antiplatelet and cardiovascular actions of a new carbacyclin derivative (ZK 36 374)--equipotent to PGI2 in vitro.
    Naunyn Schmiedebergs Arch Pharmacol. 1981 Jun;316(3):252-5 PMID: 6166877
  22. The binding of [3H]-prostacyclin to membranes of a neuronal somatic hybrid.
    Br J Pharmacol. 1981 Mar;72(3):435-41 PMID: 6266565
  23. Pharmacological and cardiovascular properties of a hydantoin derivative, BW 245 C, with high affinity and selectivity for PGD2 receptors.
    Prostaglandins. 1983 Jan;25(1):13-28 PMID: 6302737
  24. Platelet and cardiovascular activity of the hydantoin BW245C, a potent prostaglandin analogue.
    Prostaglandins. 1983 Feb;25(2):205-23 PMID: 6344147
  25. Different responsiveness of prostaglandin D2-sensitive systems to prostaglandin D2 and its analogues.
    Br J Pharmacol. 1985 Jun;85(2):367-75 PMID: 2992661
  26. Characterization of prostanoid relaxant/inhibitory receptors (psi) using a highly selective agonist, TR4979.
    Br J Pharmacol. 1986 Jan;87(1):45-56 PMID: 3006854
  27. (5Z)-carbacyclin discriminates between prostacyclin-receptors coupled to adenylate cyclase in vascular smooth muscle and platelets.
    Br J Pharmacol. 1987 Jan;90(1):255-61 PMID: 3545351
  28. Relaxation of isolated human pulmonary muscle preparations with prostacyclin (PGI2) and its analogs.
    Prostaglandins. 1987 Jun;33(6):845-54 PMID: 2445003
  29. The action of prostanoid receptor agonists and antagonists on smooth muscle and platelets.
    Br J Pharmacol. 1988 Jun;94(2):591-601 PMID: 3134971
  30. AH6809, a prostaglandin DP-receptor blocking drug on human platelets.
    Br J Pharmacol. 1988 Jul;94(3):745-54 PMID: 2460179
  31. The classification of prostaglandin DP-receptors in platelets and vasculature using BW A868C, a novel, selective and potent competitive antagonist.
    Br J Pharmacol. 1989 Feb;96(2):291-300 PMID: 2924081
  32. GR32191, a highly potent and specific thromboxane A2 receptor blocking drug on platelets and vascular and airways smooth muscle in vitro.
    Br J Pharmacol. 1989 Jul;97(3):783-94 PMID: 2527074
  33. Characterization of the prostanoid receptor profile of enprostil and isomers in smooth muscle and platelets in vitro.
    Br J Pharmacol. 1989 Dec;98(4):1335-43 PMID: 2514950
  34. Inhibitory effects of BAY u3405 on prostanoid-induced contractions in human isolated bronchial and pulmonary arterial muscle preparations.
    Br J Pharmacol. 1991 Nov;104(3):591-5 PMID: 1797322
  35. Concurrent down-regulation of IP prostanoid receptors and the alpha-subunit of the stimulatory guanine-nucleotide-binding protein (Gs) during prolonged exposure of neuroblastoma x glioma cells to prostanoid agonists. Quantification and functional implications.
    Biochem J. 1992 Jul 15;285 ( Pt 2):529-36 PMID: 1379045
  36. Prostanoid-induced relaxation of precontracted cat ciliary muscle is mediated by EP2 and DP receptors.
    Invest Ophthalmol Vis Sci. 1992 Oct;33(11):3195-201 PMID: 1328113
  37. Potentiation of aggregation and inhibition of adenylate cyclase in human platelets by prostaglandin E analogues.
    Br J Pharmacol. 1993 Feb;108(2):363-9 PMID: 8448586
  38. Cloning, functional expression, and characterization of the human prostaglandin E2 receptor EP2 subtype.
    J Biol Chem. 1994 Apr 22;269(16):11873-7 PMID: 8163486
Article Info
Journal
British journal of pharmacology
Abbr.
Br J Pharmacol
ISSN
0007-1188
DOI
10.1038/sj.bjp.0702393
Published
1999-02-00
Pages
859-66
Language
English
Region
England
NLM ID
7502536
PMCID
PMC1571232
Subset
IM
External Links
PubMed source DOI: 10.1038/sj.bjp.0702393 PMC Full Text View journal details
Analysis Services
Analysis Services

Contact

No. 2 Wenbo Road, Zhangqiu District, Jinan, Shandong

Qilu Normal University · Genelibs Bioinformatics Lab

750 Shunhua Rd, Jinan

2F, Bldg F, University Science Park

Tel: 0531-88819269

WeChat Official Account

Follow our WeChat subscription account for real-time updates and the latest in medical and biological research.


Business Email

E-mail: [email protected]

Copyright © 2026.Genelibs Jinan Honghui Biotechnology Co., Ltd. 鲁ICP备20007159号-2