Please use this identifier to cite or link to this item: https://ahro.austin.org.au/austinjspui/handle/1/13280
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dc.contributor.authorBurrell, Louise M-
dc.contributor.authorPhillips, P A-
dc.contributor.authorStephenson, J-
dc.contributor.authorRisvanis, John-
dc.contributor.authorHutchins, A M-
dc.contributor.authorJohnston, Colin I-
dc.date.accessioned2015-05-16T03:06:14Z
dc.date.available2015-05-16T03:06:14Z
dc.date.issued1993-08-01-
dc.identifier.citationThe Journal of Endocrinology; 138(2): 259-66en_US
dc.identifier.otherPUBMEDen
dc.identifier.urihttps://ahro.austin.org.au/austinjspui/handle/1/13280en
dc.description.abstractA non-peptide, orally effective, vasopressin (AVP) V1 receptor antagonist 1-(1-[4-(3-acetylaminopropoxy) benzoyl]-4-piperidyl)-3,4-dihydro-2(1H)-quinolinone (OPC-21268) has recently been described. This paper reports the in-vitro and in-vivo characterization of OPC-21268 binding to vasopressin receptors in rat liver and kidney. OPC-21268 caused a concentration-dependent displacement of the selective V1 receptor antagonist radioligand, 125I-labelled [d(CH2)5,sarcosine7]AVP to V1 receptors in both rat liver and kidney medulla membranes. The concentration of OPC-21268 that displaced 50% of specific AVP binding (IC50) was 40 +/- 3 nmol/l for liver V1 and 15 +/- 2 nmol/l for kidney V1 receptors (mean +/- S.E.M.; n = 3). OPC-21268 had little effect on the selective V2 antagonist radioligand [3H]desGly-NH2(9)]d(CH2)5,D-Ile2,Ile4] AVP binding to V2 receptors in renal medulla membranes (IC50 > 0.1 mmol/l). After oral administration to rats, OPC-21268 was an effective V1 antagonist in a time- and dose-dependent manner. Binding kinetic studies showed that OPC-21268 acted as a competitive antagonist at the liver V1 receptor in vitro and in vivo, in addition to its in-vitro competitive effects at the renal V1 receptor. OPC-21268 shows promise as an orally active V1 antagonist.en_US
dc.language.isoenen
dc.subject.otherAnimalsen
dc.subject.otherAntidiuretic Hormone Receptor Antagonistsen
dc.subject.otherArginine Vasopressin.metabolismen
dc.subject.otherDose-Response Relationship, Drugen
dc.subject.otherFemaleen
dc.subject.otherIn Vitro Techniquesen
dc.subject.otherKidney Medulla.metabolismen
dc.subject.otherLiver.metabolismen
dc.subject.otherPiperidines.pharmacologyen
dc.subject.otherProtein Bindingen
dc.subject.otherQuinolones.pharmacologyen
dc.subject.otherRadioligand Assayen
dc.subject.otherRatsen
dc.subject.otherRats, Sprague-Dawleyen
dc.subject.otherTime Factorsen
dc.titleCharacterization of a novel non-peptide vasopressin V1 receptor antagonist (OPC-21268) in the rat.en_US
dc.typeJournal Articleen_US
dc.identifier.journaltitleThe Journal of Endocrinologyen_US
dc.identifier.affiliationMedicine (University of Melbourne)en_US
dc.description.pages259-66en
dc.relation.urlhttps://pubmed.ncbi.nlm.nih.gov/8228734en
dc.type.contentTexten_US
dc.type.austinJournal Articleen
local.name.researcherBurrell, Louise M
item.openairetypeJournal Article-
item.cerifentitytypePublications-
item.grantfulltextnone-
item.fulltextNo Fulltext-
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
item.languageiso639-1en-
crisitem.author.deptCardiology-
crisitem.author.deptGeneral Medicine-
crisitem.author.deptMedicine (University of Melbourne)-
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