Source:http://linkedlifedata.com/resource/pubmed/id/10896116
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
6
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pubmed:dateCreated |
2000-12-6
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pubmed:abstractText |
In the course of our study to find an ideal antihypertensive potassium channel opener (KCO), N-(2-cyanoethyl)-2,2-bis(fluoromethyl)-6-pentafluoroethyl-2H-1-ben zopyran-4-carboxamide (13f, KC-515) showed a highly potent, slow and long-lasting antihypertensive effect with reduced reflex tachycardia, together with the beneficial effects of KCO such as improvement in lipid metabolism. These profiles identify KC-515 as a potential candidate. In conscious spontaneously hypertensive rats (SHR), the onset of the hypotensive effect of KC-515 (13f) was gradual and the maximum response was attained at around 6 h after dosing. The duration of action was over 18 h for 0.1 mg/kg. When administered to Zucker rats for 2 weeks with 0.03-0.3 mg/kg po range in the antihypertensive doses in hypertensive rat models, KC-515 (13f) significantly and dose-dependently reduced serum triglycerides to less than 70% of control without affecting total cholesterol.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
0968-0896
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
8
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1393-405
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:10896116-Animals,
pubmed-meshheading:10896116-Antihypertensive Agents,
pubmed-meshheading:10896116-Benzopyrans,
pubmed-meshheading:10896116-Hypolipidemic Agents,
pubmed-meshheading:10896116-Magnetic Resonance Spectroscopy,
pubmed-meshheading:10896116-Male,
pubmed-meshheading:10896116-Potassium Channels,
pubmed-meshheading:10896116-Rats,
pubmed-meshheading:10896116-Rats, Inbred SHR,
pubmed-meshheading:10896116-Rats, Sprague-Dawley,
pubmed-meshheading:10896116-Rats, Zucker,
pubmed-meshheading:10896116-Spectrometry, Mass, Electrospray Ionization,
pubmed-meshheading:10896116-Structure-Activity Relationship
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pubmed:year |
2000
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pubmed:articleTitle |
6-Substituted 2,2-bis(fluoromethyl)-benzopyran-4-carboxamide K+ channel openers.
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pubmed:affiliation |
Fuji-gotemba Research Laboratories, Chugai Pharmaceutical Co., Ltd., Gotemba, Shizuoka, Japan. takanok@chugai.pharm.co.jp
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pubmed:publicationType |
Journal Article
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