| pubmed-article:8331552 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:8331552 | lifeskim:mentions | umls-concept:C0033262 | lld:lifeskim |
| pubmed-article:8331552 | lifeskim:mentions | umls-concept:C0001128 | lld:lifeskim |
| pubmed-article:8331552 | lifeskim:mentions | umls-concept:C1979963 | lld:lifeskim |
| pubmed-article:8331552 | lifeskim:mentions | umls-concept:C0521942 | lld:lifeskim |
| pubmed-article:8331552 | lifeskim:mentions | umls-concept:C0205464 | lld:lifeskim |
| pubmed-article:8331552 | lifeskim:mentions | umls-concept:C2003903 | lld:lifeskim |
| pubmed-article:8331552 | lifeskim:mentions | umls-concept:C0205250 | lld:lifeskim |
| pubmed-article:8331552 | lifeskim:mentions | umls-concept:C1611588 | lld:lifeskim |
| pubmed-article:8331552 | lifeskim:mentions | umls-concept:C0174494 | lld:lifeskim |
| pubmed-article:8331552 | lifeskim:mentions | umls-concept:C0217087 | lld:lifeskim |
| pubmed-article:8331552 | pubmed:issue | 1 | lld:pubmed |
| pubmed-article:8331552 | pubmed:dateCreated | 1993-8-19 | lld:pubmed |
| pubmed-article:8331552 | pubmed:abstractText | The angiotensin II (AII) antagonistic action of 2-ethoxy-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl-1H-benzi mid azole-7 - carboxylic acid (CV-11974) was examined in in vitro assay systems, including AII receptor binding assay using membrane fractions of bovine adrenal cortex or rabbit aorta and AII-induced contraction assay using rabbit aortic strips, and CV-11974 and its prodrug, (+/-)1-(cyclohexyloxycarbonyloxy)ethyl 2-ethoxy-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H- benzimidazole-7-carboxylate (TCV-116), were examined in an in vivo system of AII-induced pressor response in conscious rats. DuP 753 or EXP3174 (the main active metabolite of DuP 753) was used as the reference compound. CV-11974 inhibited the binding of [125I] AII to the bovine adrenal cortical membrane and rabbit aortic membrane with IC50 values of 1.12 x 10(-7) and 2.86 x 10(-8) M, respectively. Similar results were obtained with EXP3174. CV-11974 interacted with AII in these membrane fractions with subtype 1 receptor in a competitive manner. CV-11974 at 10(-5) M did not affect the binding of [125I]AII to subtype 2 (AT2) receptor in bovine cerebellum. CV-11974 selectively inhibited the AII-induced contraction of rabbit aortic strips in a noncompetitive manner (pD' 2, 9.97); it had no effects on the contraction induced by norepinephrine, KCl, serotonin, prostaglandin F2 alpha or endothelin. EXP3174 showed a pD'2 value of 8.95 for the AII-induced contraction. CV-11974 given intravenously and TCV-116 given orally inhibited the AII-induced pressor response in rats with ID50 values of 0.033 mg/kg and 0.069 mg/kg, respectively. These effects of CV-11974 and TCV-116 were 12 and 48 times more potent than those of EXP3174 and DuP 753, respectively.(ABSTRACT TRUNCATED AT 250 WORDS) | lld:pubmed |
| pubmed-article:8331552 | pubmed:language | eng | lld:pubmed |
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| pubmed-article:8331552 | pubmed:citationSubset | IM | lld:pubmed |
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| pubmed-article:8331552 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:8331552 | pubmed:month | Jul | lld:pubmed |
| pubmed-article:8331552 | pubmed:issn | 0022-3565 | lld:pubmed |
| pubmed-article:8331552 | pubmed:author | pubmed-author:InadaYY | lld:pubmed |
| pubmed-article:8331552 | pubmed:author | pubmed-author:WadaTT | lld:pubmed |
| pubmed-article:8331552 | pubmed:author | pubmed-author:NishikawaKK | lld:pubmed |
| pubmed-article:8331552 | pubmed:author | pubmed-author:ShiboutaYY | lld:pubmed |
| pubmed-article:8331552 | pubmed:author | pubmed-author:KuboKK | lld:pubmed |
| pubmed-article:8331552 | pubmed:author | pubmed-author:NodaMM | lld:pubmed |
| pubmed-article:8331552 | pubmed:author | pubmed-author:OjimaMM | lld:pubmed |
| pubmed-article:8331552 | pubmed:author | pubmed-author:NakaTT | lld:pubmed |
| pubmed-article:8331552 | pubmed:author | pubmed-author:KoharaYY | lld:pubmed |
| pubmed-article:8331552 | pubmed:author | pubmed-author:SanadaTT | lld:pubmed |
| pubmed-article:8331552 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:8331552 | pubmed:volume | 266 | lld:pubmed |
| pubmed-article:8331552 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:8331552 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:8331552 | pubmed:pagination | 114-20 | lld:pubmed |
| pubmed-article:8331552 | pubmed:dateRevised | 2010-11-18 | lld:pubmed |
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| pubmed-article:8331552 | pubmed:year | 1993 | lld:pubmed |
| pubmed-article:8331552 | pubmed:articleTitle | Pharmacological profile of a highly potent and long-acting angiotensin II receptor antagonist, 2-ethoxy-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4- yl]methyl]-1H-benzimidazole-7-carboxylic acid (CV-11974), and its prodrug, (+/-)-1-(cyclohexyloxycarbonyloxy)-ethyl 2-ethoxy-1-[[2'-(1H-tetrazol-5- yl)biphenyl-4-yl]methyl]-1H-benzimidazole-7-carboxylate (TCV-116). | lld:pubmed |
| pubmed-article:8331552 | pubmed:affiliation | Pharmaceutical Research Laboratories I, Takeda Chemical Industries, Ltd., Osaka, Japan. | lld:pubmed |
| pubmed-article:8331552 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:8331552 | pubmed:publicationType | Comparative Study | lld:pubmed |
| pubmed-article:8331552 | pubmed:publicationType | In Vitro | lld:pubmed |
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