Please use this identifier to cite or link to this item: https://ahro.austin.org.au/austinjspui/handle/1/13407
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dc.contributor.authorPhillips, P Aen
dc.contributor.authorRisvanis, Johnen
dc.contributor.authorAldred, K Len
dc.contributor.authorBurrell, Louise Men
dc.contributor.authorBartholomeusz, Ben
dc.date.accessioned2015-05-16T03:15:07Z
dc.date.available2015-05-16T03:15:07Z
dc.date.issued1995-12-01en
dc.identifier.citationClinical Science 1995; 89(6): 575-9en
dc.identifier.govdoc8549075en
dc.identifier.otherPUBMEDen
dc.identifier.urihttp://ahro.austin.org.au/austinjspui/handle/1/13407en
dc.description.abstract1. We studied the effects of the non-selective, non-peptide, orally active endothelin (ET) receptor antagonist bosentan (Ro 47-0203) on rat hepatic and mesenteric vascular membrane 125I-ET-1 binding characteristics in vitro and ex vivo (after bosentan by gavage in vivo). 2. Bosentan caused a concentration-dependent competitive inhibition of 125I-ET-1 binding to female rat mesenteric vascular (predominantly ETA receptors) and hepatic (predominantly ETB receptors) membranes in vitro and ex vivo. 3. The time course of the inhibition of binding ex vivo after administration of bosentan in vivo was 1-4h for mesenteric vascular (predominantly ETA receptors) binding and 1-16h for hepatic (predominantly ETB receptors) binding. 4. The time course of displacement of 125I-ET-1 binding from mesenteric vascular and hepatic membranes by bosentan in vitro was similar. 5. Since bosentan is significantly excreted by the liver, the prolonged hepatic 125I-ET-1 binding by bosentan presumably represents hepatic accumulation of bosentan, which may have implications for bosentan antagonizing the actions of ET in the liver.en
dc.language.isoenen
dc.subject.otherAnimalsen
dc.subject.otherEndothelin Receptor Antagonistsen
dc.subject.otherEndothelins.metabolismen
dc.subject.otherFemaleen
dc.subject.otherLiver.blood supplyen
dc.subject.otherMesenteric Arteries.chemistry.drug effectsen
dc.subject.otherMesenteric Veins.chemistry.drug effectsen
dc.subject.otherRatsen
dc.subject.otherRats, Inbred WKYen
dc.subject.otherReceptors, Endothelin.metabolismen
dc.subject.otherSulfonamides.pharmacologyen
dc.titleDifferential effects of a novel non-peptide endothelin receptor antagonist (bosentan) in rat liver and vasculature.en
dc.typeJournal Articleen
dc.identifier.journaltitleClinical Scienceen
dc.identifier.affiliationDepartment of Medicine, University of Melbourne, Austin Hospital, Heidelberg, Victoria, Australiaen
dc.description.pages575-9en
dc.relation.urlhttps://pubmed.ncbi.nlm.nih.gov/8549075en
dc.type.austinJournal Articleen
item.cerifentitytypePublications-
item.languageiso639-1en-
item.grantfulltextnone-
item.openairetypeJournal Article-
item.fulltextNo Fulltext-
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
crisitem.author.deptCardiology-
crisitem.author.deptGeneral Medicine-
crisitem.author.deptMedicine (University of Melbourne)-
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