Please use this identifier to cite or link to this item: https://ahro.austin.org.au/austinjspui/handle/1/13217
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dc.contributor.authorLiu, J Jen
dc.contributor.authorPhillips, P Aen
dc.contributor.authorBurrell, Louise Men
dc.contributor.authorBuxton, Brian Fen
dc.contributor.authorJohnston, Colin Ien
dc.date.accessioned2015-05-16T03:01:43Z
dc.date.available2015-05-16T03:01:43Z
dc.date.issued1994-02-01en
dc.identifier.citationClinical and Experimental Pharmacology & Physiology; 21(2): 121-4en
dc.identifier.govdoc8039263en
dc.identifier.otherPUBMEDen
dc.identifier.urihttp://ahro.austin.org.au/austinjspui/handle/1/13217en
dc.description.abstract1. OPC-21268 and OPC-31260 are newly developed orally active non-peptide vasopressin (AVP) V1 and V2 receptor antagonists, respectively. The effects of the two compounds on human vessels have not been studied. 2. The effects of the two compounds on AVP-induced contraction of human internal mammary arteries (IMA) were investigated. Their effects were compared with the peptide V1 and V2 antagonists d(CH2)5Sar7AVP (SAVP) and d(CH2)5D-Ileu2Ileu4AVP (Ileu2Ileu4AVP), respectively. 3. The V1 antagonist OPC-21268 failed to antagonize AVP-induced contraction at low concentrations and potentiated the contraction at higher concentration (3 x 10(-7) mol/L, P < 0.05). It also caused a mild direct contractile effect on IMA. In contrast, the peptide V1 antagonist SAVP potently inhibited the AVP-induced contraction, indicating that functionally constrictor V1 receptors exist in IMA. Both the nonpeptide and peptide V2 antagonists OPC-31260 (3 x 10(-6) mol/L) and Ileu2Ileu4AVP significantly antagonized the AVP-induced contraction (P < 0.01). 4. The AVP-induced contraction was reversed by high concentrations of OPC-31260 (10(-6) mol/L-3 x 10(-5) mol/L) but not by OPC-21268 (up to 3 x 10(-5) mol/L). 5. These studies indicate that, in human IMA, OPC-21268 is a partial V1 receptor agonist with no V1 receptor antagonist activity, while OPC-31260 is a V1 receptor antagonist. The results also indicate that Ileu2Ileu4AVP may be a V1 receptor antagonist in humans.en
dc.language.isoenen
dc.subject.otherAntidiuretic Hormone Receptor Antagonistsen
dc.subject.otherArginine Vasopressin.analogs & derivatives.antagonists & inhibitors.pharmacologyen
dc.subject.otherArteries.drug effectsen
dc.subject.otherBenzazepines.pharmacologyen
dc.subject.otherBreast.blood supplyen
dc.subject.otherFemaleen
dc.subject.otherHumansen
dc.subject.otherIn Vitro Techniquesen
dc.subject.otherMuscle Contraction.drug effectsen
dc.subject.otherMuscle, Smooth, Vascular.drug effectsen
dc.subject.otherNorepinephrine.pharmacologyen
dc.subject.otherPiperidines.pharmacologyen
dc.subject.otherQuinolones.pharmacologyen
dc.subject.otherReceptors, Vasopressin.drug effectsen
dc.subject.otherRegional Blood Flow.drug effectsen
dc.titleHuman internal mammary artery responses to non-peptide vasopressin antagonists.en
dc.typeJournal Articleen
dc.identifier.journaltitleClinical and Experimental Pharmacology & Physiologyen
dc.identifier.affiliationDepartment of Cardiac Surgery, University of Melbourne, Austin Hospital, Heidelberg, Victoria, Australiaen
dc.description.pages121-4en
dc.relation.urlhttps://pubmed.ncbi.nlm.nih.gov/8039263en
dc.type.austinJournal Articleen
item.languageiso639-1en-
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
item.openairetypeJournal Article-
item.grantfulltextnone-
item.cerifentitytypePublications-
item.fulltextNo Fulltext-
crisitem.author.deptCardiology-
crisitem.author.deptGeneral Medicine-
crisitem.author.deptMedicine (University of Melbourne)-
crisitem.author.deptCardiac Surgery-
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