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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
17
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pubmed:dateCreated |
1998-9-9
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pubmed:abstractText |
Substituted 1,4-benzoxazines bearing an amino side chain at the 2-position were prepared and were found to have a moderate activity on intracellular calcium. Of the compounds studied it was found that those which possess a homoveratrylamino moiety exhibited superior potency. The chain length and the nature of the amine (4-fluorophenylpiperazine, 4-fluorobenzhydryloxyethylamine, N-substituted homoveratrylamine) is discussed. The 4-benzyl-3, 4-dihydro-2-[3-[[2-(3,4-dimethoxyphenyl)ethyl]amino]propyl]-2H-1, 4-benzoxazine (3c) is the most potent derivative of the series with a ratio of IC50 values against PE (phenylephrine) and K+ of 2.1. Under these test conditions a ratio near 1 indicates potential intracellular calcium activity while a ratio greater than 100 an action on extracellular calcium influx.
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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 |
Aug
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
13
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pubmed:volume |
41
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pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
3142-58
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:9703461-Animals,
pubmed-meshheading:9703461-Aorta,
pubmed-meshheading:9703461-Calcium,
pubmed-meshheading:9703461-Calcium Channel Blockers,
pubmed-meshheading:9703461-Drug Design,
pubmed-meshheading:9703461-Male,
pubmed-meshheading:9703461-Molecular Structure,
pubmed-meshheading:9703461-Muscle, Smooth, Vascular,
pubmed-meshheading:9703461-Muscle Contraction,
pubmed-meshheading:9703461-Oxazines,
pubmed-meshheading:9703461-Phenylephrine,
pubmed-meshheading:9703461-Rabbits,
pubmed-meshheading:9703461-Renal Artery,
pubmed-meshheading:9703461-Second Messenger Systems,
pubmed-meshheading:9703461-Structure-Activity Relationship,
pubmed-meshheading:9703461-Vasoconstriction
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pubmed:year |
1998
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pubmed:articleTitle |
New substituted 1,4-benzoxazine derivatives with potential intracellular calcium activity.
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pubmed:affiliation |
Institut de Chimie Organique et Analytique associé au CNRS, Université d'Orléans, BP 6759, 45067 Orléans Cedex 2, France.
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pubmed:publicationType |
Journal Article,
In Vitro
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