Source:http://linkedlifedata.com/resource/pubmed/id/20947677
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
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pubmed:dateCreated |
2011-5-2
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pubmed:abstractText |
Pulmonary arterial hypertension (PAH) is a life-threatening disease characterised by vasoconstriction and remodelling of the pulmonary vasculature. The serotonin (5-hydroxytryptamine (5-HT)) pathway has been shown to play a major role in the pathogenesis of PAH, but pharmacological modulation of this pathway for treatment of PAH is, to date, at a pre-clinical level. Terguride is a 5-HT receptor (5-HTR) antagonist that is well tolerated and clinically approved for ovulation disorders. Immunohistochemistry against 5-HTR(?A/B) on human lungs revealed their localisation to the vascular smooth muscle layer and quantitative RT-PCR showed 5-HTR(?B) upregulation in pulmonary artery smooth muscle cells (PASMC) isolated from PAH patients. Proliferation and migration of cultured primary human PASMC were dose-dependently blocked by terguride. Therapeutic 5-HT signalling inhibition was 1) demonstrated in isolated, ventilated and perfused rat lungs and 2) by chronic terguride treatment of rats with monocrotaline (MCT)-induced pulmonary hypertension in a preventive or curative approach. Terguride inhibited proliferation of PASMCs and abolished 5-HT-induced pulmonary vasoconstriction. Chronic terguride treatment prevented dose-dependently the development and progression of MCT-induced PAH in rats. Thus, terguride represents a valuable novel therapeutic approach in PAH.
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pubmed:commentsCorrections | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Dopamine Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Lisuride,
http://linkedlifedata.com/resource/pubmed/chemical/Monocrotaline,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin 5-HT2 Receptor Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/dironyl
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
1399-3003
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pubmed:author |
pubmed-author:DumitrascuRR,
pubmed-author:EickelbergOO,
pubmed-author:GhofraniH AHA,
pubmed-author:GrimmingerFF,
pubmed-author:KönigshoffMM,
pubmed-author:KouraNN,
pubmed-author:KulckeCC,
pubmed-author:MorrellNN,
pubmed-author:PullamsettiS SSS,
pubmed-author:ReiterRR,
pubmed-author:SchermulyR TRT,
pubmed-author:SeegerWW,
pubmed-author:WeissmannNN,
pubmed-author:YangXX
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pubmed:issnType |
Electronic
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pubmed:volume |
37
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1104-18
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pubmed:dateRevised |
2011-11-15
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pubmed:meshHeading |
pubmed-meshheading:20947677-Adult,
pubmed-meshheading:20947677-Animals,
pubmed-meshheading:20947677-Cell Proliferation,
pubmed-meshheading:20947677-Cells, Cultured,
pubmed-meshheading:20947677-Dopamine Agonists,
pubmed-meshheading:20947677-Female,
pubmed-meshheading:20947677-Humans,
pubmed-meshheading:20947677-Hypertension, Pulmonary,
pubmed-meshheading:20947677-Lisuride,
pubmed-meshheading:20947677-Lung,
pubmed-meshheading:20947677-Lung Transplantation,
pubmed-meshheading:20947677-Male,
pubmed-meshheading:20947677-Monocrotaline,
pubmed-meshheading:20947677-Muscle, Smooth, Vascular,
pubmed-meshheading:20947677-Pulmonary Artery,
pubmed-meshheading:20947677-Rats,
pubmed-meshheading:20947677-Serotonin 5-HT2 Receptor Antagonists
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pubmed:year |
2011
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pubmed:articleTitle |
Terguride ameliorates monocrotaline-induced pulmonary hypertension in rats.
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pubmed:affiliation |
University of Giessen Lung Center, Germany.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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