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Expression and functional evidence of the prostaglandin F2alpha receptor mediating contraction in human umbilical vein.
- Source :
-
European journal of pharmacology [Eur J Pharmacol] 2009 May 21; Vol. 610 (1-3), pp. 68-74. Date of Electronic Publication: 2009 Mar 14. - Publication Year :
- 2009
-
Abstract
- Our purposes were to perform the pharmacological characterization of PGF(2alpha) receptor (prostanoid FP-receptor) involved in human umbilical vein contraction and confirm its expression in this tissue. Umbilical cords from healthy patients after full-term deliveries were employed. The vein was dissected out of cords and used for either isolated organ bath or reverse transcription-polymerase chain reaction (RT-PCR) and Western blot assays. The natural prostanoid FP-receptor agonist, PGF(2alpha), and its selective analogues, latanoprost and bimatoprost free acids are full agonists (produce more than 80% of the maximal contractile response to 5-HT) in human umbilical vein. The agonist potency (pEC(50)) order was PGF(2alpha) (6.01+/-0.05)>latanoprost free acid (5.65+/-0.07)=bimatoprost free acid (5.59+/-0.08). The contractile effects of PGF(2alpha) and latanoprost free acid were blocked competitively by the prostanoid FP-receptor antagonist, AL-8810. The antagonist potencies (pK(B)) of AL-8810 vs. PGF(2alpha) (5.93+/-0.05) and vs. latanoprost free acid (6.40+/-0.08) in human umbilical vein are in good agreement with its ability to antagonize prostanoid FP receptors of rat, mouse and human cells. In all samples, clear signal was detected for cDNA amplification of prostanoid FP receptor and the specific prostanoid FP-receptor antibody recognized a protein of approximately 64 kDa. In conclusion, taking into account the obtained functional and biochemical data, we propose for the first time that human umbilical vein express prostanoid FP-receptors and these receptors could be involved in the vasoconstriction action of PGF(2alpha) in this tissue.
- Subjects :
- Amides agonists
Bimatoprost
Cloprostenol agonists
Cloprostenol analogs & derivatives
Dinoprost agonists
Dose-Response Relationship, Drug
Endothelium, Vascular metabolism
Gene Expression drug effects
Humans
Infant, Newborn
Latanoprost
Muscle, Smooth, Vascular drug effects
Muscle, Smooth, Vascular metabolism
Prostaglandins F, Synthetic agonists
Receptors, Prostaglandin agonists
Umbilical Veins cytology
Umbilical Veins metabolism
Receptors, Prostaglandin metabolism
Umbilical Veins drug effects
Vasoconstriction drug effects
Vasoconstrictor Agents pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1879-0712
- Volume :
- 610
- Issue :
- 1-3
- Database :
- MEDLINE
- Journal :
- European journal of pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 19289115
- Full Text :
- https://doi.org/10.1016/j.ejphar.2009.03.022