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https://ahro.austin.org.au/austinjspui/handle/1/13280
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DC Field | Value | Language |
---|---|---|
dc.contributor.author | Burrell, Louise M | - |
dc.contributor.author | Phillips, P A | - |
dc.contributor.author | Stephenson, J | - |
dc.contributor.author | Risvanis, John | - |
dc.contributor.author | Hutchins, A M | - |
dc.contributor.author | Johnston, Colin I | - |
dc.date.accessioned | 2015-05-16T03:06:14Z | |
dc.date.available | 2015-05-16T03:06:14Z | |
dc.date.issued | 1993-08-01 | - |
dc.identifier.citation | The Journal of Endocrinology; 138(2): 259-66 | en_US |
dc.identifier.other | PUBMED | en |
dc.identifier.uri | https://ahro.austin.org.au/austinjspui/handle/1/13280 | en |
dc.description.abstract | A 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.iso | en | en |
dc.subject.other | Animals | en |
dc.subject.other | Antidiuretic Hormone Receptor Antagonists | en |
dc.subject.other | Arginine Vasopressin.metabolism | en |
dc.subject.other | Dose-Response Relationship, Drug | en |
dc.subject.other | Female | en |
dc.subject.other | In Vitro Techniques | en |
dc.subject.other | Kidney Medulla.metabolism | en |
dc.subject.other | Liver.metabolism | en |
dc.subject.other | Piperidines.pharmacology | en |
dc.subject.other | Protein Binding | en |
dc.subject.other | Quinolones.pharmacology | en |
dc.subject.other | Radioligand Assay | en |
dc.subject.other | Rats | en |
dc.subject.other | Rats, Sprague-Dawley | en |
dc.subject.other | Time Factors | en |
dc.title | Characterization of a novel non-peptide vasopressin V1 receptor antagonist (OPC-21268) in the rat. | en_US |
dc.type | Journal Article | en_US |
dc.identifier.journaltitle | The Journal of Endocrinology | en_US |
dc.identifier.affiliation | Medicine (University of Melbourne) | en_US |
dc.description.pages | 259-66 | en |
dc.relation.url | https://pubmed.ncbi.nlm.nih.gov/8228734 | en |
dc.type.content | Text | en_US |
dc.type.austin | Journal Article | en |
local.name.researcher | Burrell, Louise M | |
item.openairetype | Journal Article | - |
item.cerifentitytype | Publications | - |
item.grantfulltext | none | - |
item.fulltext | No Fulltext | - |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.languageiso639-1 | en | - |
crisitem.author.dept | Cardiology | - |
crisitem.author.dept | General Medicine | - |
crisitem.author.dept | Medicine (University of Melbourne) | - |
Appears in Collections: | Journal articles |
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