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Article: Effect of short- and long-acting β2-adrenoceptor agonists on pulmonary β2-adrenoceptor expression in human lung

TitleEffect of short- and long-acting β2-adrenoceptor agonists on pulmonary β2-adrenoceptor expression in human lung
Authors
Issue Date1996
PublisherElsevier BV. The Journal's web site is located at http://www.elsevier.com/locate/ejphar
Citation
European Journal Of Pharmacology, 1996, v. 318 n. 1, p. 123-129 How to Cite?
Abstractβ-Adrenoceptor agonists induce the down-regulation of β2-adrenoceptors and mRNA expression in animal lung. The down-regulation of β2-adrenoceptors may limit the therapeutic efficacy of β2-adrenoceptor-mediated bronchodilators in obstructive airways disease. We examined the effects of three selective β2-adrenoceptor agonists, salbutamol, salmeterol and formoterol on β2-adrenoceptor binding and mRNA levels in human lung in vitro. Human lung was obtained from cardiac transplantation donors. Peripheral lung was chopped and incubated with three selective β2-adrenoceptor agonist for 3 h or 24 h at three different concentrations (0.1, 1 and 10 μM). The affinity and density of β2-adrenoceptors was determined by [125I]iodocyanopindolol equilibrium binding in a lung membrane preparation in the presence of 0.1 μM CGP 20712 A (1-{2-[(3-carbamoyl-4-hydroxy)phenoxy]ethylamino}-3-[4-(1-methyl-4 -trifluoromethyl-2-imidazolyl)phenoxy]-propan-2-ol), a selective β1-adrenoceptor antagonist. Although treatment with salbutamol for 3 h did not change β2-adrenoceptor density, both salmeterol and formoterol reduced β2-adrenoceptor density, and exposure to each agonist for 24 h reduced β2-adrenoceptor density at all concentrations. Treatment with 10 μM salmeterol increased the equilibrium dissociation constant (K(d)), and also shifted the competition curves of (-)-isoprenaline to the left. β2-Adrenoceptor mRNA, measured by Northern blot analysis using a human β2-adrenoceptor cDNA probe, was reduced after exposure to all β2-adrenoceptor agonists at 3 h. Our data provide evidence for down-regulation of β2-adrenoceptor protein and mRNA after selective β2-adrenoceptor agonist treatment in human lung.
Persistent Identifierhttp://hdl.handle.net/10722/162167
ISSN
2015 Impact Factor: 2.73
2015 SCImago Journal Rankings: 1.115
ISI Accession Number ID
References

 

DC FieldValueLanguage
dc.contributor.authorNishikawa, Men_US
dc.contributor.authorMak, JCWen_US
dc.contributor.authorBarnes, PJen_US
dc.date.accessioned2012-09-05T05:17:46Z-
dc.date.available2012-09-05T05:17:46Z-
dc.date.issued1996en_US
dc.identifier.citationEuropean Journal Of Pharmacology, 1996, v. 318 n. 1, p. 123-129en_US
dc.identifier.issn0014-2999en_US
dc.identifier.urihttp://hdl.handle.net/10722/162167-
dc.description.abstractβ-Adrenoceptor agonists induce the down-regulation of β2-adrenoceptors and mRNA expression in animal lung. The down-regulation of β2-adrenoceptors may limit the therapeutic efficacy of β2-adrenoceptor-mediated bronchodilators in obstructive airways disease. We examined the effects of three selective β2-adrenoceptor agonists, salbutamol, salmeterol and formoterol on β2-adrenoceptor binding and mRNA levels in human lung in vitro. Human lung was obtained from cardiac transplantation donors. Peripheral lung was chopped and incubated with three selective β2-adrenoceptor agonist for 3 h or 24 h at three different concentrations (0.1, 1 and 10 μM). The affinity and density of β2-adrenoceptors was determined by [125I]iodocyanopindolol equilibrium binding in a lung membrane preparation in the presence of 0.1 μM CGP 20712 A (1-{2-[(3-carbamoyl-4-hydroxy)phenoxy]ethylamino}-3-[4-(1-methyl-4 -trifluoromethyl-2-imidazolyl)phenoxy]-propan-2-ol), a selective β1-adrenoceptor antagonist. Although treatment with salbutamol for 3 h did not change β2-adrenoceptor density, both salmeterol and formoterol reduced β2-adrenoceptor density, and exposure to each agonist for 24 h reduced β2-adrenoceptor density at all concentrations. Treatment with 10 μM salmeterol increased the equilibrium dissociation constant (K(d)), and also shifted the competition curves of (-)-isoprenaline to the left. β2-Adrenoceptor mRNA, measured by Northern blot analysis using a human β2-adrenoceptor cDNA probe, was reduced after exposure to all β2-adrenoceptor agonists at 3 h. Our data provide evidence for down-regulation of β2-adrenoceptor protein and mRNA after selective β2-adrenoceptor agonist treatment in human lung.en_US
dc.languageengen_US
dc.publisherElsevier BV. The Journal's web site is located at http://www.elsevier.com/locate/ejpharen_US
dc.relation.ispartofEuropean Journal of Pharmacologyen_US
dc.subject.meshAdolescenten_US
dc.subject.meshAdrenergic Beta-Agonists - Pharmacologyen_US
dc.subject.meshAdulten_US
dc.subject.meshAlbuterol - Analogs & Derivatives - Pharmacologyen_US
dc.subject.meshBinding Sitesen_US
dc.subject.meshBinding, Competitiveen_US
dc.subject.meshBlotting, Northernen_US
dc.subject.meshDown-Regulationen_US
dc.subject.meshEthanolamines - Pharmacologyen_US
dc.subject.meshHumansen_US
dc.subject.meshIsoproterenol - Pharmacologyen_US
dc.subject.meshLung - Drug Effects - Metabolismen_US
dc.subject.meshMaleen_US
dc.subject.meshRna, Messenger - Analysisen_US
dc.subject.meshReceptors, Adrenergic, Beta-2 - Biosynthesis - Drug Effectsen_US
dc.titleEffect of short- and long-acting β2-adrenoceptor agonists on pulmonary β2-adrenoceptor expression in human lungen_US
dc.typeArticleen_US
dc.identifier.emailMak, JCW:judymak@hku.hken_US
dc.identifier.authorityMak, JCW=rp00352en_US
dc.description.naturelink_to_subscribed_fulltexten_US
dc.identifier.doi10.1016/S0014-2999(96)00769-8en_US
dc.identifier.pmid9007523-
dc.identifier.scopuseid_2-s2.0-0030604281en_US
dc.relation.referenceshttp://www.scopus.com/mlt/select.url?eid=2-s2.0-0030604281&selection=ref&src=s&origin=recordpageen_US
dc.identifier.volume318en_US
dc.identifier.issue1en_US
dc.identifier.spage123en_US
dc.identifier.epage129en_US
dc.identifier.isiWOS:A1996WB93700020-
dc.publisher.placeNetherlandsen_US
dc.identifier.scopusauthoridNishikawa, M=7402607361en_US
dc.identifier.scopusauthoridMak, JCW=7103323094en_US
dc.identifier.scopusauthoridBarnes, PJ=36064679400en_US

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