Pharmacological characterization of prostanoid receptors mediating vasoconstriction in human umbilical vein

Daray, Federico Manuel; Minvielle, Ana Itatí; Puppo, Soledad; Rothlin, Rodolfo Pedro

doi:10.1038/sj.bjp.0705375

Cited by 21 publications

(11 citation statements)

References 41 publications

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“…This is consistent with a stimulatory action of PGE 2 on TP receptors. The PGE 2 promiscuous interaction with TP receptors, especially at concentrations higher than 1 M, has also been observed in several vascular tissues including human umbilical arteries (Boersma et al 1999) and veins (Daray et al 2003), human uterine arteries (Baxter et al 1995) and aorta of the spontaneously hypertensive rat (Tang et al 2008). An alternative explanation for the eVects of SQ29,548 on PGE2-induced relaxation might be the blockade of a baseline TxA2-or isoprostaneinduced tone (Gonzalez-Luis et al 2005), allowing greater relaxatory actions of PGE on its dilatory receptors.…”

Section: Discussionmentioning

confidence: 80%

Developmental changes in the effects of prostaglandin E2 in the chicken ductus arteriosus

et al. 2008

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Prostaglandin E 2 (PGE 2 ) is the major vasodilator prostanoid of the mammalian ductus arteriosus (DA). In the present study we analyzed the response of isolated DA rings from 15-, 19-and 21-day-old chicken embryos to PGE 2 and other vascular smooth muscle relaxing agents acting through the cyclic AMP signaling pathway. PGE 2 exhibited a relaxant response in the 15-day DA, but not in the 19-and 21-day DA. Moreover, high concentrations of PGE 2 (¸3 M in 15-day and ¸1 M in 19-day and 21-day DA) induced contraction of the chicken DA. The presence of the TP receptor antagonist SQ29,548, unmasked a relaxant eVect of PGE 2 in the 19-and 21-day DA and increased the relaxation induced by PGE 2 in the 15-day DA. The presence of the EP receptor antagonist AH6809 abolished PGE 2 -mediated relaxation. The relaxant responses induced by PGE 2 and the -adrenoceptor agonist isoproterenol, but not those elicited by the adenylate cyclase activator forskolin or the phosphodiesterase 3 inhibitor milrinone, decreased with maturation. High oxygen concentrations (95%) decreased the relaxation to PGE 2 . The relaxing potency and eYcacy of isoproterenol and milrinone were higher in the pulmonary than in the aortic side of the DA, whereas no regional diVerences were found in the response to PGE 2 . We conclude that, in contrast to the mammalian situation, PGE 2 is a weak relaxant agent of the chicken DA and, with advancing incubation, it even stimulates TP vasoconstrictive receptors.

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Section: Discussionmentioning

confidence: 80%

Developmental changes in the effects of prostaglandin E2 in the chicken ductus arteriosus

et al. 2008

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“…Thus, when a functional study is performed using ring preparations, the circular layer is the one evaluated, whereas the longitudinal layer is tested using longitudinal strips segments and both layers using helical strips segments. In previous reports, significant differences in potency or efficacy of several vasoactive agents were observed between rings and strips preparation of HUV ( Rogines‐Velo et al ., 2002b ; Daray et al ., 2003 ). Hence, the anatomical differences described regarding the tissue preparations employed provides an explanation for the pharmacological differences observed between the results published by Altura et al .…”

Section: Discussionmentioning

confidence: 99%

Pharmacological characterization of muscarinic receptor subtypes mediating vasoconstriction of human umbilical vein

Pujol-Lereis

Hita

Gobbi

et al. 2006

British J Pharmacology

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1 The present study attempted to pharmacologically characterize the muscarinic receptor subtypes mediating contraction of human umbilical vein (HUV). 2 HUV rings were mounted in organ baths and concentration-response curves were constructed for acetylcholine (ACh) (pEC 50 : 6.1670.04; maximum response 80.0071.98% of the responses induced by serotonin 10 mM). The absence of endothelium did not modify the contractile responses of ACh in this tissue. 3 The role of cholinesterases was evaluated: neither neostigmine (acetylcholinesterase inhibitor) nor iso-OMPA (butyrylcholinesterase inhibitor) modified ACh responses. When both enzymes were simultaneously inhibited, a significantly but little potentiation was observed (control: pEC 50 6.3370.03; double inhibition: pEC 50 6.5770.05). 4 Atropine, nonselective muscarinic receptors antagonist, inhibited ACh-induced contraction (pK B 9.67). The muscarinic receptors antagonists pirenzepine (M 1 ), methoctramine (M 2 ) and pFHHSiD (M 3 ) also antagonized responses to ACh. The affinity values estimated for these antagonists against responses evoked by ACh were 7.58, 6.78 and 7.94, respectively. On the other hand, PD 102807 (M 4 selective muscarinic receptors antagonist) was ineffective against ACh-induced contraction. 5 In presence of a blocking concentration of pirenzepine, pFHHSiFD produced an additional antagonism activity on ACh-induced responses. 6 The M 1 muscarinic receptors agonist McN-A-343 produced similar maximum but less potent responses than ACh in HUV. The calculated pA 2 for pirenzepine against McN-A-343 induced responses was 8.54. 7 In conclusion, the data obtained in this study demonstrate the role of M 1 muscarinic receptor subtypes and suggest the involvement of M 3 muscarinic receptor subtypes in ACh-induced vasoconstriction in HUV rings. In addition, the vasomotor activity evoked by ACh does not seem to be modulated by endothelial factors, and their enzymatic degradation appears to have little functional relevance in this tissue.

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“…Thus, it is a useful drug tool for characterization of PG E receptors [318]. The effect of AH6809 (11) has been studied upon the anti-aggregatory and aggregatory actions of various agents in human blood platelets.…”

Section: Ah6809 a Prostaglandin Receptor Antagonistmentioning

confidence: 99%

Xanthone Derivatives: New Insights in Biological Activities

Pinto¹,

Sousa

Nascimento

2005

CMC

450

232

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Xanthones or xanthen-9H-ones (dibenzo-gamma-pirone) comprise an important class of oxygenated heterocycles whose role is well-known in Medicinal Chemistry. The biological activities of this class of compounds are associated with their tricyclic scaffold but vary depending on the nature and/or position of the different substituents. In this review, an array of biological/pharmacological effects is presented for both natural and synthetic xanthone derivatives, with an emphasis on some significant studies on structure-activity relationships. The antitumor activity of some xanthones as well as the related targets, particularly PKC modulation studies, is also discussed in detail. Examples of the "hit" compounds involved in cancer therapy, namely DMXAA, psorospermin, mangiferin, norathyriol, mangostins, and AH6809, a prostanoid receptor antagonist, are also mentioned. Finally, a historical perspective of these xanthonic derivatives, their relevance as therapeutic agents and/or their uses as pharmacological tools and as extract components in folk medicine are also highlighted.

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Pharmacological characterization of prostanoid receptors mediating vasoconstriction in human umbilical vein

Cited by 21 publications

References 41 publications

Developmental changes in the effects of prostaglandin E2 in the chicken ductus arteriosus

Developmental changes in the effects of prostaglandin E2 in the chicken ductus arteriosus

Pharmacological characterization of muscarinic receptor subtypes mediating vasoconstriction of human umbilical vein

Xanthone Derivatives: New Insights in Biological Activities

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