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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
1989-8-30
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pubmed:abstractText |
In our continuing search for low molecular weight, human renin inhibitors, a dipeptide derivative, morpholino-naphthyl-acyl-histidyl-cyclohexyl-norstatine (KRI-1314), was newly synthesized and estimated for oral effectiveness. This compound inhibited plasma renin from humans and from Japanese monkeys in vitro, with 50% inhibitory concentrations (IC50) of 4.7 x 10(-9) and 2.4 x 10(-8) mol/l, respectively. The mean blood pressure of sodium-depleted Japanese monkeys was lowered significantly after intravenous injection or oral administration of KRI-1314. The maximum reduction was attained 3 h after oral administration at a dose of 10 mg/kg. Plasma renin activity (PRA) was halved 1 h after oral administration of KRI-1314, and this inhibition persisted for more than 5 h. results suggest that KRI-1314, a potent, orally effective and long-lasting renin inhibitor, may become one of a new class of antihypertensive agent.
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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/Antihypertensive Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Dipeptides,
http://linkedlifedata.com/resource/pubmed/chemical/Morpholines,
http://linkedlifedata.com/resource/pubmed/chemical/Naphthalenes,
http://linkedlifedata.com/resource/pubmed/chemical/Renin,
http://linkedlifedata.com/resource/pubmed/chemical/Sodium
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
0952-1178
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
7
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
S25-7
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:2666609-Administration, Oral,
pubmed-meshheading:2666609-Animals,
pubmed-meshheading:2666609-Antihypertensive Agents,
pubmed-meshheading:2666609-Blood Pressure,
pubmed-meshheading:2666609-Dipeptides,
pubmed-meshheading:2666609-Female,
pubmed-meshheading:2666609-Humans,
pubmed-meshheading:2666609-Hypertension,
pubmed-meshheading:2666609-Macaca,
pubmed-meshheading:2666609-Male,
pubmed-meshheading:2666609-Morpholines,
pubmed-meshheading:2666609-Naphthalenes,
pubmed-meshheading:2666609-Renin,
pubmed-meshheading:2666609-Sodium
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pubmed:year |
1989
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pubmed:articleTitle |
An orally active renin inhibitor: cyclohexylnorstatine-containing dipeptide (KRI-1314).
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pubmed:affiliation |
Department of Pharmacology, Osaka Medical College, Japan.
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pubmed:publicationType |
Journal Article
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