Please use this identifier to cite or link to this item: https://ahro.austin.org.au/austinjspui/handle/1/9187
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dc.contributor.authorRisvanis, Johnen
dc.contributor.authorNaitoh, Men
dc.contributor.authorJohnston, Colin Ien
dc.contributor.authorBurrell, Louise Men
dc.date.accessioned2015-05-15T22:11:00Z
dc.date.available2015-05-15T22:11:00Z
dc.date.issued1999-09-17en
dc.identifier.citationEuropean Journal of Pharmacology; 381(1): 23-30en
dc.identifier.govdoc10528130en
dc.identifier.otherPUBMEDen
dc.identifier.urihttps://ahro.austin.org.au/austinjspui/handle/1/9187en
dc.description.abstractThis paper reports the in vitro and in vivo characterisation of a nonpeptide, orally active, vasopressin V(1A) and V(2) receptor antagonist, YM087 (methyl-1,4,5,6-tetrahydroimidazo[4, 5-d][1]benzoazepine-6-carbonyl)-2-phenylbenzanilide monohydrochloride) in the rat. YM087 dose dependently displaced the vasopressin V(1A) receptor antagonist radioligand, 125I-labelled [d(CH(2))(5),sarcosine(7)]vasopressin at vasopressin V(1A) receptors in liver and kidney medulla membranes and caused a concentration dependent displacement of the vasopressin V(2) receptor antagonist radioligand [3H]desGly-NH(2)(9)[d(CH(2))(5), D-Ile(2), Ile(4)]vasopressin at vasopressin V(2) receptors in kidney medulla membranes. In vitro binding kinetic studies showed YM087 acted as a competitive antagonist at liver V(1A) and kidney V(1A) and V(2) vasopressin receptors. Oral administration of YM087 (0.1-3 mg/kg) dose dependently inhibited vasopressin binding to liver V(1A) and kidney V(1A) and V(2) vasopressin receptors over 24 h. Oral YM087 (1-3 mg/kg/day) for 7 days in normotensive rats caused a dose dependent aquaresis with no effect on systolic blood pressure. These results show that YM087 is an orally effective vasopressin V(1A) and V(2) receptor antagonist that may be useful in the treatment of conditions characterised by vasoconstriction and fluid retention such as congestive heart failure.en
dc.language.isoenen
dc.subject.otherAdministration, Oralen
dc.subject.otherAnimalsen
dc.subject.otherAntidiuretic Hormone Receptor Antagonistsen
dc.subject.otherBenzazepines.metabolism.pharmacologyen
dc.subject.otherBinding, Competitive.drug effectsen
dc.subject.otherBlood Pressure.drug effectsen
dc.subject.otherDose-Response Relationship, Drugen
dc.subject.otherIodine Radioisotopes.diagnostic useen
dc.subject.otherKidney.drug effects.metabolismen
dc.subject.otherKineticsen
dc.subject.otherLiver.drug effects.metabolismen
dc.subject.otherMaleen
dc.subject.otherMembranes.drug effects.metabolismen
dc.subject.otherRadioligand Assayen
dc.subject.otherRatsen
dc.subject.otherRats, Sprague-Dawleyen
dc.subject.otherSodium.blood.urineen
dc.subject.otherSystoleen
dc.subject.otherUrination.drug effectsen
dc.subject.otherVasopressins.metabolismen
dc.titleIn vivo and in vitro characterisation of a nonpeptide vasopressin V(1A) and V(2) receptor antagonist (YM087) in the rat.en
dc.typeJournal Articleen
dc.identifier.journaltitleEuropean Journal of Pharmacologyen
dc.identifier.affiliationDepartment of Medicine, The University of Melbourne, Austin and Repatriation Medical Centre, Heidelberg, Victoria 3084, Australiaen
dc.description.pages23-30en
dc.relation.urlhttps://pubmed.ncbi.nlm.nih.gov/10528130en
dc.type.austinJournal Articleen
local.name.researcherBurrell, Louise M
item.grantfulltextnone-
item.fulltextNo Fulltext-
item.cerifentitytypePublications-
item.languageiso639-1en-
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
item.openairetypeJournal Article-
crisitem.author.deptCardiology-
crisitem.author.deptGeneral Medicine-
crisitem.author.deptMedicine (University of Melbourne)-
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