Please use this identifier to cite or link to this item: https://ahro.austin.org.au/austinjspui/handle/1/9142
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dc.contributor.authorLouis, Simon N Sen
dc.contributor.authorNero, Tracy Len
dc.contributor.authorIakovidis, Den
dc.contributor.authorJackman, G Pen
dc.contributor.authorLouis, William Jen
dc.date.accessioned2015-05-15T22:07:02Z
dc.date.available2015-05-15T22:07:02Z
dc.date.issued1999-02-19en
dc.identifier.citationEuropean Journal of Pharmacology; 367(2-3): 431-5en
dc.identifier.govdoc10079020en
dc.identifier.otherPUBMEDen
dc.identifier.urihttp://ahro.austin.org.au/austinjspui/handle/1/9142en
dc.description.abstractLK 204-545 ((+/-)-1-(2-(3-(2-cyano-4-(2-cyclopropyl-methoxy-ethoxy)phenoxy)-2-hydro xy-propyl-amino)-ethyl)-3-(4-hydrxy-phenyl) urea), an antagonist that possesses high beta1-/beta2-selectivity in the rat, and a range of cardio-selective and non-selective beta-adrenoceptor antagonists were examined to compare their radioligand binding affinities for human beta1-, beta2- and beta3-adrenoceptors transfected into CHO cells. LK 204-545 and CGP 20712A displayed the highest beta1-/beta2- (approximately 1800 and approximately 650, respectively) and beta1-/beta3-selectivity (approximately 17000 and approximately 2200, respectively) at human beta-adrenoceptors with LK 204-545 being approximately 2.75-fold more beta1-/beta2-selective and approximately 8-fold beta1-/beta3-selective than CGP 20712A. The high potency of LK 204-545 at transfected human beta1-adrenoceptors and in functional models of rat beta1-adrenoceptors together with its high selectivity, identify it as a useful ligand for studying beta1-adrenoceptors and suggest that it may be the preferred ligand for human beta-adrenoceptor studies.en
dc.language.isoenen
dc.subject.otherAdrenergic beta-Agonists.metabolismen
dc.subject.otherAdrenergic beta-Antagonists.metabolism.pharmacologyen
dc.subject.otherAnimalsen
dc.subject.otherCHO Cellsen
dc.subject.otherCricetinaeen
dc.subject.otherCyclopropanes.pharmacologyen
dc.subject.otherFemaleen
dc.subject.otherHumansen
dc.subject.otherImidazoles.metabolismen
dc.subject.otherIn Vitro Techniquesen
dc.subject.otherLigandsen
dc.subject.otherPhenoxypropanolaminesen
dc.subject.otherProtein Bindingen
dc.subject.otherRatsen
dc.subject.otherRats, Sprague-Dawleyen
dc.subject.otherReceptors, Adrenergic, beta.metabolismen
dc.subject.otherReceptors, Adrenergic, beta-1.metabolismen
dc.subject.otherReceptors, Adrenergic, beta-2.metabolismen
dc.subject.otherTrachea.physiologyen
dc.subject.otherUrea.analogs & derivatives.pharmacologyen
dc.titleLK 204-545, a highly selective beta1-adrenoceptor antagonist at human beta-adrenoceptors.en
dc.typeJournal Articleen
dc.identifier.journaltitleEuropean Journal of Pharmacologyen
dc.identifier.affiliationDepartment of Clinical Pharmacology and Therapeutics Unit, The University of Melbourne, Austin and Repatriation Medical Centre, Heidelberg, Victoria, Australiaen
dc.description.pages431-5en
dc.relation.urlhttps://pubmed.ncbi.nlm.nih.gov/10079020en
dc.type.austinJournal Articleen
item.cerifentitytypePublications-
item.languageiso639-1en-
item.grantfulltextnone-
item.openairetypeJournal Article-
item.fulltextNo Fulltext-
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
crisitem.author.deptClinical Pharmacology and Therapeutics-
Appears in Collections:Journal articles
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