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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
15
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pubmed:dateCreated |
1995-9-12
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pubmed:abstractText |
BA 41899 (5-methyl-6-phenyl-1,3,5,6-tetrahydro-3,6-methano-1,5- benzodiazocine-2,4-dione, 6) is a structurally novel 1,5-benzodiazocine derivative and represents the prototype of a hitherto unknown class of positive inotropic Ca(2+)-sensitizing agents. It is completely devoid of phosphodiesterase (PDE) III inhibitory activity or any other known inotropic mechanism. BA 41899 (6) exhibits a pharmacological in vitro profile comprising Ca(2+)-sensitizing, positive inotropic, and negative chronotropic effects. CGP 48506 ((+)-6), the (+)-enantiomer of BA 41899 (6), enantiospecifically carries Ca2+ sensitization by up to a full pCa unit and a corresponding positive inotropic effect. Conversely, the negative chronotropic action resides in the corresponding (-)-enantiomer, CGP 48508 ((-)-6). All the effects are exerted in the low micromolar range. The positive inotropic action of CGP 48506 ((+)-6) is associated with a decelerating effect on contraction and, more prominently, relaxation dynamics in isolated guinea pig atria. In contrast to Ca(2+)-sensitizing PDE inhibitors, CGP 48506 ((+)-6) does not increase maximum Ca(2+)-activated force in myocardial skinned fibers.
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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/Azocines,
http://linkedlifedata.com/resource/pubmed/chemical/Calcium,
http://linkedlifedata.com/resource/pubmed/chemical/Cardiotonic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Imidazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Phosphodiesterase Inhibitors
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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:day |
21
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pubmed:volume |
38
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2946-54
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
pubmed-meshheading:7636855-Animals,
pubmed-meshheading:7636855-Azocines,
pubmed-meshheading:7636855-Calcium,
pubmed-meshheading:7636855-Cardiotonic Agents,
pubmed-meshheading:7636855-Electric Stimulation,
pubmed-meshheading:7636855-Guinea Pigs,
pubmed-meshheading:7636855-Heart Atria,
pubmed-meshheading:7636855-Heart Failure,
pubmed-meshheading:7636855-Imidazoles,
pubmed-meshheading:7636855-Isometric Contraction,
pubmed-meshheading:7636855-Myocardial Contraction,
pubmed-meshheading:7636855-Myocardium,
pubmed-meshheading:7636855-Phosphodiesterase Inhibitors,
pubmed-meshheading:7636855-Sensitivity and Specificity,
pubmed-meshheading:7636855-Stereoisomerism,
pubmed-meshheading:7636855-Swine
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pubmed:year |
1995
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pubmed:articleTitle |
5-Methyl-6-phenyl-1,3,5,6-tetrahydro-3,6-methano-1,5-benzodiazocine-2,4-dione (BA 41899): representative of a novel class of purely calcium-sensitizing agents.
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pubmed:affiliation |
Cardiovascular Research Department, Ciba-Geigy Limited, Basel, Switzerland.
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pubmed:publicationType |
Journal Article,
Comparative Study,
In Vitro
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