rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
15
|
pubmed:dateCreated |
2002-7-12
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pubmed:abstractText |
Three novel metabolites of the angiotensin-II (A-II) receptor antagonist tasosartan have been identified in humans, and the syntheses and pharmacologic profiling of these metabolites are reported. Each metabolite bound the human A-II receptor with IC(50)s between 20 and 45nM. The in vivo effects of these compounds in attenuating the pressor response to angiotensin-II challenge in anesthetized rats were also investigated. An unsaturated diol metabolite exhibited in vivo efficacy at intravenous doses of 1 and 3mg/kg, while the other metabolites, both carboxylic acids, had no significant effect at the same doses.
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pubmed:language |
eng
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pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Aug
|
pubmed:issn |
0960-894X
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:day |
5
|
pubmed:volume |
12
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
1967-71
|
pubmed:dateRevised |
2010-11-18
|
pubmed:meshHeading |
pubmed-meshheading:12113820-Angiotensin Receptor Antagonists,
pubmed-meshheading:12113820-Animals,
pubmed-meshheading:12113820-Blood Pressure,
pubmed-meshheading:12113820-Dose-Response Relationship, Drug,
pubmed-meshheading:12113820-Heart Rate,
pubmed-meshheading:12113820-Humans,
pubmed-meshheading:12113820-Inhibitory Concentration 50,
pubmed-meshheading:12113820-Injections, Intravenous,
pubmed-meshheading:12113820-Pyrimidines,
pubmed-meshheading:12113820-Rats,
pubmed-meshheading:12113820-Receptors, Angiotensin,
pubmed-meshheading:12113820-Structure-Activity Relationship,
pubmed-meshheading:12113820-Tetrazoles
|
pubmed:year |
2002
|
pubmed:articleTitle |
Novel human metabolites of the angiotensin-II antagonist tasosartan and their pharmacological effects.
|
pubmed:affiliation |
Medicinal Chemistry, Chemical Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543, USA. elokdah@wyeth.com
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pubmed:publicationType |
Journal Article
|