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Article: Raloxifene relaxes rat pulmonary arteries and veins: Roles of gender, endothelium, and antagonism of Ca2+ influx

TitleRaloxifene relaxes rat pulmonary arteries and veins: Roles of gender, endothelium, and antagonism of Ca2+ influx
Authors
Issue Date2005
PublisherAmerican Society for Pharmacology and Experimental Therapeutics. The Journal's web site is located at http://jpet.aspetjournals.org
Citation
Journal Of Pharmacology And Experimental Therapeutics, 2005, v. 312 n. 3, p. 1266-1271 How to Cite?
AbstractEffects of raloxifene have been documented in the systemic circulation. However, its impact on the pulmonary circulation is unclear. The present study investigated the role of gender, endothelial modulation, and Ca2+ channel in relaxations evoked by raloxifene in rat pulmonary arteries and veins. Vascular responses were studied on isolated pulmonary blood vessels mounted in a myograph and constricted by U46619 (9,11-dideoxy-11α,9α- epoxymethanoprostaglandin F2α). Constrictions to CaCl 2 were studied in Ca2+-free, 60 mM K+ solution. Changes in the intracellular calcium ion concentration ([Ca2+] i) in vascular smooth muscle were measured using a calcium fluorescence imaging method. Raloxifene was more effective in relaxing U46619-constricted pulmonary arteries from male than female rats. Raloxifene-induced relaxation was unaffected by ICI 182,780 [7α-[9-[(4,4, 5,5,5,-pentafluoropentyl)-sulfinyl]nonyl]-estra-1,3,5(10)-triene-3, 17β-diol], inhibition of the nitric oxide (NO) pathway, or removal of the endothelium. In arteries without endothelium, raloxifene attenuated CaCl 2-induced constriction and CaCl2-stimulated increase in [Ca2+]i with similar potencies. Raloxifene caused endothelium-independent relaxations in pulmonary veins, albeit to a lesser degree than in pulmonary arteries. The venous responses showed a gender difference because raloxifene was more potent in male veins. In summary, raloxifene relaxed rat pulmonary arteries, and this effect did not involve the endothelium/NO or ICI 182,780-sensitive estrogen receptors. Raloxifene, like nifedipine, reduced constriction and [Ca2+]i increase in response to CaCl2 in high K+ solution. Raloxifene also relaxed high K+-constricted pulmonary veins. Our data indicate that raloxifene acutely relaxes rat pulmonary blood vessels primarily via inhibition of Ca2+ influx through voltage-sensitive Ca2+ channels. Finally, raloxifene induced more relaxation in blood vessels isolated from male than female rats. Copyright © 2005 by The American Society for Pharmacology and Experimental Therapeutics.
Persistent Identifierhttp://hdl.handle.net/10722/134682
ISSN
2015 Impact Factor: 3.76
2015 SCImago Journal Rankings: 1.847
ISI Accession Number ID
References

 

DC FieldValueLanguage
dc.contributor.authorChan, YCen_HK
dc.contributor.authorLeung, FPen_HK
dc.contributor.authorYao, Xen_HK
dc.contributor.authorLau, CWen_HK
dc.contributor.authorVanhoutte, PMen_HK
dc.contributor.authorHuang, Yen_HK
dc.date.accessioned2011-07-05T08:24:18Z-
dc.date.available2011-07-05T08:24:18Z-
dc.date.issued2005en_HK
dc.identifier.citationJournal Of Pharmacology And Experimental Therapeutics, 2005, v. 312 n. 3, p. 1266-1271en_HK
dc.identifier.issn0022-3565en_HK
dc.identifier.urihttp://hdl.handle.net/10722/134682-
dc.description.abstractEffects of raloxifene have been documented in the systemic circulation. However, its impact on the pulmonary circulation is unclear. The present study investigated the role of gender, endothelial modulation, and Ca2+ channel in relaxations evoked by raloxifene in rat pulmonary arteries and veins. Vascular responses were studied on isolated pulmonary blood vessels mounted in a myograph and constricted by U46619 (9,11-dideoxy-11α,9α- epoxymethanoprostaglandin F2α). Constrictions to CaCl 2 were studied in Ca2+-free, 60 mM K+ solution. Changes in the intracellular calcium ion concentration ([Ca2+] i) in vascular smooth muscle were measured using a calcium fluorescence imaging method. Raloxifene was more effective in relaxing U46619-constricted pulmonary arteries from male than female rats. Raloxifene-induced relaxation was unaffected by ICI 182,780 [7α-[9-[(4,4, 5,5,5,-pentafluoropentyl)-sulfinyl]nonyl]-estra-1,3,5(10)-triene-3, 17β-diol], inhibition of the nitric oxide (NO) pathway, or removal of the endothelium. In arteries without endothelium, raloxifene attenuated CaCl 2-induced constriction and CaCl2-stimulated increase in [Ca2+]i with similar potencies. Raloxifene caused endothelium-independent relaxations in pulmonary veins, albeit to a lesser degree than in pulmonary arteries. The venous responses showed a gender difference because raloxifene was more potent in male veins. In summary, raloxifene relaxed rat pulmonary arteries, and this effect did not involve the endothelium/NO or ICI 182,780-sensitive estrogen receptors. Raloxifene, like nifedipine, reduced constriction and [Ca2+]i increase in response to CaCl2 in high K+ solution. Raloxifene also relaxed high K+-constricted pulmonary veins. Our data indicate that raloxifene acutely relaxes rat pulmonary blood vessels primarily via inhibition of Ca2+ influx through voltage-sensitive Ca2+ channels. Finally, raloxifene induced more relaxation in blood vessels isolated from male than female rats. Copyright © 2005 by The American Society for Pharmacology and Experimental Therapeutics.en_HK
dc.languageengen_US
dc.publisherAmerican Society for Pharmacology and Experimental Therapeutics. The Journal's web site is located at http://jpet.aspetjournals.orgen_HK
dc.relation.ispartofJournal of Pharmacology and Experimental Therapeuticsen_HK
dc.subject.meshAnimalsen_HK
dc.subject.meshCalcium - metabolismen_HK
dc.subject.meshCalcium Channels, L-Type - physiologyen_HK
dc.subject.meshDose-Response Relationship, Drugen_HK
dc.subject.meshEndothelium, Vascular - physiologyen_HK
dc.subject.meshEstradiol - analogs & derivatives - pharmacologyen_HK
dc.subject.meshFemaleen_HK
dc.subject.meshMaleen_HK
dc.subject.meshPulmonary Artery - drug effects - physiologyen_HK
dc.subject.meshPulmonary Veins - drug effects - physiologyen_HK
dc.subject.meshRaloxifene - pharmacologyen_HK
dc.subject.meshRatsen_HK
dc.subject.meshRats, Sprague-Dawleyen_HK
dc.subject.meshSelective Estrogen Receptor Modulators - pharmacologyen_HK
dc.subject.meshSex Characteristicsen_HK
dc.subject.meshVasodilation - drug effectsen_HK
dc.titleRaloxifene relaxes rat pulmonary arteries and veins: Roles of gender, endothelium, and antagonism of Ca2+ influxen_HK
dc.typeArticleen_HK
dc.identifier.emailChan, YC:yauchi@graduate.hku.hken_US
dc.identifier.authorityChan, YC=rp01502en_US
dc.description.naturelink_to_subscribed_fulltexten_US
dc.identifier.doi10.1124/jpet.104.077990en_HK
dc.identifier.pmid15550571-
dc.identifier.scopuseid_2-s2.0-14344263790en_HK
dc.identifier.hkuros155342-
dc.identifier.hkuros136333-
dc.relation.referenceshttp://www.scopus.com/mlt/select.url?eid=2-s2.0-14344263790&selection=ref&src=s&origin=recordpageen_HK
dc.identifier.volume312en_HK
dc.identifier.issue3en_HK
dc.identifier.spage1266en_HK
dc.identifier.epage1271en_HK
dc.identifier.isiWOS:000227008800046-
dc.publisher.placeUnited Statesen_HK
dc.identifier.scopusauthoridChan, YC=7403676116-
dc.identifier.scopusauthoridLeung, FP=8615375300-
dc.identifier.scopusauthoridYao, X=7402529434-
dc.identifier.scopusauthoridLau, CW=7401968520-
dc.identifier.scopusauthoridVanhoutte, PM=7202304247-
dc.identifier.scopusauthoridHuang, Y=7501573013-

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