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Predicate | Object |
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rdf:type | |
lifeskim:mentions |
umls-concept:C0007209,
umls-concept:C0205314,
umls-concept:C0205464,
umls-concept:C0220781,
umls-concept:C0243072,
umls-concept:C0260181,
umls-concept:C0439849,
umls-concept:C0445223,
umls-concept:C0456387,
umls-concept:C0679622,
umls-concept:C0871161,
umls-concept:C1552599,
umls-concept:C1704787,
umls-concept:C1883254
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pubmed:issue |
7
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pubmed:dateCreated |
1987-8-7
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pubmed:abstractText |
A series of [4-(substituted-amino)phenyl]pyridazinones and [4-(substituted-methyl)amino]phenyl]pyridazinones was synthesized and evaluated for inotropic activity in vitro and for cardiohemodynamic effects in vivo. Above all, 6-[4-(4-pyridylamino)phenyl]-4,5-dihydro-3(2H)-pyridazinone hydrochloride (4, MCI-154) and 6-[4-(4-pyridylamino)phenyl]-5-methyl-4,5-dihydro-3(2H)-pyridazinone hydrochloride (5) showed extremely potent positive inotropic activity along with vasodilating activity. Regarding dP/dtmax (an indicator for cardiac contractility), ED30's (doses that increased dP/dtmax by 30%) of compounds 4 and 5 were 8.5 +/- 1.9 and 4.4 +/- 0.6 micrograms/kg, respectively, where that of amrinone was 471.9 +/- 94.1 micrograms/kg. Structure-activity relationships of these series are presented, and a plausible model of receptor binding is discussed.
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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 |
Jul
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
30
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1157-61
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:3599022-Animals,
pubmed-meshheading:3599022-Cardiotonic Agents,
pubmed-meshheading:3599022-Dogs,
pubmed-meshheading:3599022-Female,
pubmed-meshheading:3599022-Male,
pubmed-meshheading:3599022-Models, Molecular,
pubmed-meshheading:3599022-Myocardial Contraction,
pubmed-meshheading:3599022-Structure-Activity Relationship
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pubmed:year |
1987
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pubmed:articleTitle |
A novel class of cardiotonics. Synthesis and pharmacological properties of [4-(substituted-amino)phenyl]pyridazinones and related derivatives.
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pubmed:publicationType |
Journal Article
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