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Article: Celiprolol has no direct or indirect relaxing effects in isolated arteries and veins

TitleCeliprolol has no direct or indirect relaxing effects in isolated arteries and veins
Authors
Issue Date1990
PublisherLippincott Williams & Wilkins. The Journal's web site is located at http://www.cardiovascularpharm.com/
Citation
Journal Of Cardiovascular Pharmacology, 1990, v. 15 n. 5, p. 831-835 How to Cite?
AbstractExperiments were designed to study the potential mechanisms underlying the vasodilator effect of celiprolol. Rings of canine left circumflex coronary artery and rat mesenteric artery, with and without endothelium, were suspended in organ chambers for isometric tension recording. In both blood vessels, celiprolol (10-9-10-4 M) failed to produce relaxation in rings with and without endothelium; these same tissues relaxed in an endothelium-dependent manner to acetylcholine (10-6 M). All tissues relaxed completely in the presence of papaverine (10-4 M). In the coronary artery, isoproterenol (10-9-10-4 M) produced endothelium-independent relaxations which were inhibited in a competitive fashion by celiprolol (pA2 = 7.52 + 0.14; slope = 0.98, 95% confidence limits = 0.80-1.15). In other experiments, strips of canine saphenous veins were incubated with [3H]norepinephrine ([3H]NE) and suspended for superfusion. Electrical stimulation (2 Hz, 4 V, 2 ms for 6 min) produced an increase in [3H]NE overflow. Isoproterenol ( 2 x 10-6 M) augmented the evoked release of [3H]NE. Treatment of the strips with celipropol (up to 5 x 10-6 M) did not inhibit isoproterenol-induced facilitation of [3H]NE release. Thus, although celiprolol is a potent antagonist of postjunctional β-adrenoceptors in the coronary artery, no evidence was obtained for a direct or indirect vasodilator effect of celiprolol on isolated blood vessels.
Persistent Identifierhttp://hdl.handle.net/10722/170992
ISSN
2015 Impact Factor: 2.462
2015 SCImago Journal Rankings: 0.962
ISI Accession Number ID

 

DC FieldValueLanguage
dc.contributor.authorO'rourke, STen_US
dc.contributor.authorVanhoutte, PMen_US
dc.date.accessioned2012-10-30T06:11:45Z-
dc.date.available2012-10-30T06:11:45Z-
dc.date.issued1990en_US
dc.identifier.citationJournal Of Cardiovascular Pharmacology, 1990, v. 15 n. 5, p. 831-835en_US
dc.identifier.issn0160-2446en_US
dc.identifier.urihttp://hdl.handle.net/10722/170992-
dc.description.abstractExperiments were designed to study the potential mechanisms underlying the vasodilator effect of celiprolol. Rings of canine left circumflex coronary artery and rat mesenteric artery, with and without endothelium, were suspended in organ chambers for isometric tension recording. In both blood vessels, celiprolol (10-9-10-4 M) failed to produce relaxation in rings with and without endothelium; these same tissues relaxed in an endothelium-dependent manner to acetylcholine (10-6 M). All tissues relaxed completely in the presence of papaverine (10-4 M). In the coronary artery, isoproterenol (10-9-10-4 M) produced endothelium-independent relaxations which were inhibited in a competitive fashion by celiprolol (pA2 = 7.52 + 0.14; slope = 0.98, 95% confidence limits = 0.80-1.15). In other experiments, strips of canine saphenous veins were incubated with [3H]norepinephrine ([3H]NE) and suspended for superfusion. Electrical stimulation (2 Hz, 4 V, 2 ms for 6 min) produced an increase in [3H]NE overflow. Isoproterenol ( 2 x 10-6 M) augmented the evoked release of [3H]NE. Treatment of the strips with celipropol (up to 5 x 10-6 M) did not inhibit isoproterenol-induced facilitation of [3H]NE release. Thus, although celiprolol is a potent antagonist of postjunctional β-adrenoceptors in the coronary artery, no evidence was obtained for a direct or indirect vasodilator effect of celiprolol on isolated blood vessels.en_US
dc.languageengen_US
dc.publisherLippincott Williams & Wilkins. The Journal's web site is located at http://www.cardiovascularpharm.com/en_US
dc.relation.ispartofJournal of Cardiovascular Pharmacologyen_US
dc.subject.meshAdrenergic Beta-Antagonists - Pharmacologyen_US
dc.subject.meshAnimalsen_US
dc.subject.meshArteries - Drug Effectsen_US
dc.subject.meshCeliprololen_US
dc.subject.meshDinoprost - Pharmacologyen_US
dc.subject.meshIsometric Contractionen_US
dc.subject.meshMuscle Contraction - Drug Effectsen_US
dc.subject.meshMuscle Relaxation - Drug Effectsen_US
dc.subject.meshMuscle, Smooth, Vascular - Drug Effectsen_US
dc.subject.meshNorepinephrine - Pharmacologyen_US
dc.subject.meshPapaverine - Pharmacologyen_US
dc.subject.meshPropanolamines - Pharmacologyen_US
dc.subject.meshRatsen_US
dc.subject.meshRats, Inbred Strainsen_US
dc.subject.meshSaphenous Vein - Drug Effectsen_US
dc.subject.meshVeins - Drug Effectsen_US
dc.titleCeliprolol has no direct or indirect relaxing effects in isolated arteries and veinsen_US
dc.typeArticleen_US
dc.identifier.emailVanhoutte, PM:vanhoutt@hku.hken_US
dc.identifier.authorityVanhoutte, PM=rp00238en_US
dc.description.naturelink_to_subscribed_fulltexten_US
dc.identifier.doi10.1097/00005344-199005000-00020-
dc.identifier.pmid1692945-
dc.identifier.scopuseid_2-s2.0-0025342353en_US
dc.identifier.volume15en_US
dc.identifier.issue5en_US
dc.identifier.spage831en_US
dc.identifier.epage835en_US
dc.identifier.isiWOS:A1990DA55200020-
dc.publisher.placeUnited Statesen_US
dc.identifier.scopusauthoridO'Rourke, ST=7005313078en_US
dc.identifier.scopusauthoridVanhoutte, PM=7202304247en_US

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