Source:http://linkedlifedata.com/resource/pubmed/id/10714952
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
2000-3-29
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pubmed:abstractText |
In the present study the vasorelaxing capacity of cromakalim, an ATP-sensitive potassium-channel (KATP channel) activator, and that of levosimendan, a new positive inotropic and vasodilating drug with calcium sensitizing and potassium-channel-activating properties, were compared in human isolated portal vein. Based on the 50% effective concentrations (EC50), levosimendan was found to be about 16-fold more potent (EC50 = 0.281+/-0.03 microM) as a relaxing agent than cromakalim (EC50 = 4.53+/-0.12 microM) in noradrenaline-precontracted portal venous preparations. Glibenclamide, the known inhibitor of KATP channels, was able to prevent the cromakalim-induced venodilation completely. Glibenclamide (15 microM) decreased the quasi-maximal effect of levosimendan (at 1.27 microm by about 60%) and also the effects of those submicromolar concentrations of the inodilator (at 0.1 microM by 23%, at 0.3 microM by 27% and at 0.7 microM by 19%, on average) which were therapeutically effective in preliminary human studies. These findings indicate that, in the human portal vein, both cromakalim and levosimendan are powerful vasorelaxants and that a considerable part of the relaxing effect induced by levosimendan is of cromakalim type.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Cromakalim,
http://linkedlifedata.com/resource/pubmed/chemical/Hydrazones,
http://linkedlifedata.com/resource/pubmed/chemical/Potassium Channels,
http://linkedlifedata.com/resource/pubmed/chemical/Pyridazines,
http://linkedlifedata.com/resource/pubmed/chemical/Vasodilator Agents,
http://linkedlifedata.com/resource/pubmed/chemical/simendan
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0022-3573
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
52
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
213-7
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:10714952-Adolescent,
pubmed-meshheading:10714952-Adult,
pubmed-meshheading:10714952-Cromakalim,
pubmed-meshheading:10714952-Female,
pubmed-meshheading:10714952-Humans,
pubmed-meshheading:10714952-Hydrazones,
pubmed-meshheading:10714952-Male,
pubmed-meshheading:10714952-Middle Aged,
pubmed-meshheading:10714952-Portal Vein,
pubmed-meshheading:10714952-Potassium Channels,
pubmed-meshheading:10714952-Pyridazines,
pubmed-meshheading:10714952-Vasodilation,
pubmed-meshheading:10714952-Vasodilator Agents
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pubmed:year |
2000
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pubmed:articleTitle |
Comparison of the vasorelaxing effect of cromakalim and the new inodilator, levosimendan, in human isolated portal vein.
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pubmed:affiliation |
Department of Pharmacology and Pharmacotherapy, Albert Szent-Györgyi Medical University, Hungarian Academy of Sciences, Szeged.
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pubmed:publicationType |
Journal Article,
Comparative Study,
In Vitro,
Research Support, Non-U.S. Gov't
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