Please use this identifier to cite or link to this item: https://ahro.austin.org.au/austinjspui/handle/1/12860
Full metadata record
DC FieldValueLanguage
dc.contributor.authorJackson, Ben
dc.contributor.authorCubela, R Ben
dc.contributor.authorJohnston, Colin Ien
dc.date.accessioned2015-05-16T02:36:30Z
dc.date.available2015-05-16T02:36:30Z
dc.date.issued1988-06-01en
dc.identifier.citationThe Journal of Pharmacology and Experimental Therapeutics; 245(3): 950-5en
dc.identifier.govdoc2838609en
dc.identifier.otherPUBMEDen
dc.identifier.urihttp://ahro.austin.org.au/austinjspui/handle/1/12860en
dc.description.abstractChanges in angiotensin converting enzyme (ACE) derived from plasma, lung, aorta, brain, kidney and testis were measured in rats treated with perindopril. Angiotensin converting enzyme was measured by a radio inhibitor binding method using 125I351A. Rats were gavage fed perindopril (1, 4 and 8 mg/kg) and changes followed over 48 hr. Plasma and kidney ACE were both affected acutely with reduction of 125I351A binding to less than 5% of that in control animals 1 and 2 hr after gavage. Ligand binding to ACE in plasma and kidney returned to control levels after 24 hr. Ligand binding to ACE in lung, aorta and brain also was displaced after perindopril treatment. Changes were of a lesser degree than in plasma or kidney. Maximal effect was 1 to 4 hr after treatment and persisted through 24 hr postgavage. Ligand binding to ACE from testis was little altered over the time period of study. In a dose varying study rats were gavage fed perindopril (0-32 mg/kg) and tissues were studied 4 hr later. Ligand binding to plasma and kidney ACE was displaced by 50% at a dose of 1 mg/kg or less, whereas a dose of 16 to 32 mg/kg was required for a similar effect on ACE in lung, aorta and brain. ACE in testis was only affected to a small degree at a dose of 32 mg/kg. ACE is tissues was inhibited differentially after oral treatment with perindopril. Although differing in bioavailability, bioactivation of the drug or different binding properties of the enzyme could all account for the results, the most likely explanation is that there is variation in tissue penetration of the drug.en
dc.language.isoenen
dc.subject.otherAngiotensin-Converting Enzyme Inhibitors.pharmacologyen
dc.subject.otherAnimalsen
dc.subject.otherBlood Pressure.drug effectsen
dc.subject.otherDipeptides.metabolismen
dc.subject.otherIndoles.pharmacologyen
dc.subject.otherIodine Radioisotopes.diagnostic useen
dc.subject.otherMaleen
dc.subject.otherPeptidyl-Dipeptidase A.analysis.metabolismen
dc.subject.otherPerindoprilen
dc.subject.otherRadioligand Assayen
dc.subject.otherRatsen
dc.subject.otherRats, Inbred Strainsen
dc.titleInhibition of tissue angiotensin converting enzyme by perindopril: in vivo assessment in the rat using radioinhibitor binding displacement.en
dc.typeJournal Articleen
dc.identifier.journaltitleThe Journal of pharmacology and experimental therapeuticsen
dc.identifier.affiliationMelbourne University, Department of Medicine, Austin Hospital, Heidelberg, Victoria, Australiaen
dc.description.pages950-5en
dc.relation.urlhttps://pubmed.ncbi.nlm.nih.gov/2838609en
dc.type.austinJournal Articleen
item.openairetypeJournal Article-
item.fulltextNo Fulltext-
item.languageiso639-1en-
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
item.grantfulltextnone-
item.cerifentitytypePublications-
crisitem.author.deptGastroenterology and Hepatology-
Appears in Collections:Journal articles
Show simple item record

Page view(s)

6
checked on Feb 6, 2023

Google ScholarTM

Check


Items in AHRO are protected by copyright, with all rights reserved, unless otherwise indicated.