Please use this identifier to cite or link to this item: https://ahro.austin.org.au/austinjspui/handle/1/13077
Full metadata record
DC FieldValueLanguage
dc.contributor.authorTung, L Hen
dc.contributor.authorJackman, Gen
dc.contributor.authorCampbell, Ben
dc.contributor.authorLouis, Simon N Sen
dc.contributor.authorIakovidis, Den
dc.contributor.authorLouis, William Jen
dc.date.accessioned2015-05-16T02:51:25Z
dc.date.available2015-05-16T02:51:25Z
dc.date.issued1993-03-01en
dc.identifier.citationJournal of Cardiovascular Pharmacology; 21(3): 484-8en
dc.identifier.govdoc7681512en
dc.identifier.otherPUBMEDen
dc.identifier.urihttps://ahro.austin.org.au/austinjspui/handle/1/13077en
dc.description.abstractCeliprolol given intravenously (i.v.) to pithed rats in the dose range of 0.1-10,000 micrograms/g produced a dose-dependent increase in heart rate (HR) which was greatest (123 beats/min) at 1,000-3,000 micrograms/kg. This partial agonist effect was blocked by the selective beta 1-adrenoceptor antagonist CGP 20712A. Celiprolol also produced a vasodepressor effect in this dose range which was abolished by the relatively selective beta 2-adrenoceptor antagonist ICI 118551 but not CGP 20712A. The magnitude of this intrinsic sympathomimetic activity (ISA) response was not significantly altered by reserpine pretreatment. Celiprolol also antagonised the effects of isoprenaline 0.05 microgram/kg on HR and blood pressure (BP). The beta 1 selectivity of celiprolol as an antagonist in pithed rats (beta 1/beta 2 = 340:1) was similar to that observed in studies with isolated guinea pig atria and trachea (beta 1/beta 2 = 63:1), both being considerably greater than that observed with atenolol. Celiprolol, however, like atenolol, potentiated the bronchoconstrictor responses to histamine (3 micrograms/kg). Metabolic studies of rats and human urine failed to show significant amounts of potentially vasoactive metabolites. These data are consistent with celiprolol acting as both a beta 1- and beta 2- adrenoceptor partial agonist.en
dc.language.isoenen
dc.subject.otherAdrenergic beta-Antagonists.pharmacologyen
dc.subject.otherAirway Resistance.drug effectsen
dc.subject.otherAnimalsen
dc.subject.otherBlood Pressure.drug effectsen
dc.subject.otherCeliprolol.metabolism.pharmacologyen
dc.subject.otherDecerebrate Stateen
dc.subject.otherGuinea Pigsen
dc.subject.otherHeart Rate.drug effectsen
dc.subject.otherImidazoles.pharmacologyen
dc.subject.otherIn Vitro Techniquesen
dc.subject.otherPropanolamines.pharmacologyen
dc.subject.otherRatsen
dc.subject.otherRats, Sprague-Dawleyen
dc.subject.otherReceptors, Adrenergic, beta.drug effectsen
dc.titlePartial agonist activity of celiprolol.en
dc.typeJournal Articleen
dc.identifier.journaltitleJournal of Cardiovascular Pharmacologyen
dc.identifier.affiliationDepartment of Clinical Pharmacology and Therapeutics, Austin Hospital, Heidelberg, Australiaen
dc.description.pages484-8en
dc.relation.urlhttps://pubmed.ncbi.nlm.nih.gov/7681512en
dc.type.austinJournal Articleen
local.name.researcherLouis, William J
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
item.cerifentitytypePublications-
item.fulltextNo Fulltext-
item.grantfulltextnone-
item.languageiso639-1en-
item.openairetypeJournal Article-
crisitem.author.deptClinical Pharmacology and Therapeutics-
Appears in Collections:Journal articles
Show simple item record

Page view(s)

8
checked on Mar 28, 2024

Google ScholarTM

Check


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