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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
1991-3-27
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pubmed:abstractText |
A series of 11-[(omega-aminoalkanoyl)amino]-6,6a,7,8,9,10,10a,11- octahydrodibenzo[b,e]thiepin derivatives were prepared and found to be a structurally new class of calcium antagonists. The structure-activity relationship studies indicated that the optimum was (6aR*,10aR*,11R*)-11-[[4-[4-(4-fluorophenyl)-1- piperazinyl]butyryl] amino]-6,6a,7,8,9,10,10a,11-octahydrodibenzo[b,e]thiepin (31,pA2 8.16), which was superior to diltiazem (pA2 7.42) in calcium antagonistic activity. Compound 31 showed antihypertensive activity in anesthetized rats, without a significant effect on the heart rate. It had also antianginal effects in vasopressin-induced ST-depression and methacholine-induced ST-elevation testings in rats. These potencies of 31 were essentially equal to those of diltiazem.
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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 |
Feb
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
34
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
593-9
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:1995882-Animals,
pubmed-meshheading:1995882-Blood Pressure,
pubmed-meshheading:1995882-Calcium Channel Blockers,
pubmed-meshheading:1995882-Chemical Phenomena,
pubmed-meshheading:1995882-Chemistry,
pubmed-meshheading:1995882-Dibenzothiepins,
pubmed-meshheading:1995882-Heart Rate,
pubmed-meshheading:1995882-Male,
pubmed-meshheading:1995882-Rats,
pubmed-meshheading:1995882-Rats, Inbred Strains,
pubmed-meshheading:1995882-Structure-Activity Relationship
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pubmed:year |
1991
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pubmed:articleTitle |
A new class of calcium antagonists. Synthesis and biological activity of 11-[(omega-aminoalkanoyl)amino]-6,6a,7,8,9,10,10a,11-octahydrodibenzo [b,e]thiepin derivatives.
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pubmed:affiliation |
Research Laboratory, Dainippon Pharmaceutical Co., Ltd., Osaka, Japan.
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pubmed:publicationType |
Journal Article
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