pubmed-article:7498322 | rdf:type | pubmed:Citation | lld:pubmed |
pubmed-article:7498322 | lifeskim:mentions | umls-concept:C0031330 | lld:lifeskim |
pubmed-article:7498322 | lifeskim:mentions | umls-concept:C0001128 | lld:lifeskim |
pubmed-article:7498322 | lifeskim:mentions | umls-concept:C0529330 | lld:lifeskim |
pubmed-article:7498322 | lifeskim:mentions | umls-concept:C0231491 | lld:lifeskim |
pubmed-article:7498322 | pubmed:issue | 1-3 | lld:pubmed |
pubmed-article:7498322 | pubmed:dateCreated | 1996-1-18 | lld:pubmed |
pubmed-article:7498322 | pubmed:abstractText | The angiotensin II antagonistic activity of SB 203220, [E-alpha-[[2-butyl-1-(4-carboxy-1-naphthalenyl)methyl]-1H- imidazol-5-yl]-methylene]-2-thiophene-propanic acid], was examined in several in vitro and in vivo assays. SB 203220 displaced [125I]angiotensin II binding from a variety of tissues including the cloned human AT1 receptor (IC(50)5-15 nM). SB 203220 (10 microM) did not interact with AT2, endothelin (ETA and ETB) or calcitonin gene-related peptide receptors. [3H]SB 203220 bound with high affinity to the AT1 receptor (Kd = 4.9 nM), but dissociated from the receptor at a much slower rate when compared to [3H]SK&F 108566. SB 203220 antagonized intracellular Ca2+ mobilization induced by angiotensin II in rat vascular smooth muscle cells and exhibited a selective and partially insurmountable antagonism of angiotensin II-induced contraction in isolated rabbit aorta. In the aorta, SB 203220 produced a concentration-dependent parallel shift in the concentration-response curve to angiotensin II [EC30 = 5.94 +/- 1.6 10(-11) M] and depressed the maximal contractile response to angiotensin II by approximately 35%. The antagonistic effect of SB 203220 in rabbit aorta was slowly reversible compared to SK&F 108566. SB 203220 displayed no agonist activity and had no effect on the contractile responses to KCl, endothelin-1 or norepinephrine. In rats, SB 203220 at 10 mg/kg i.v. inhibited angiotensin II-induced aldosterone release. Intraduodenal or oral administration of SB 203220 (1-10 mg/kg) to conscious rats and dogs inhibited the pressor responses to exogenous angiotensin II.(ABSTRACT TRUNCATED AT 250 WORDS) | lld:pubmed |
pubmed-article:7498322 | pubmed:language | eng | lld:pubmed |
pubmed-article:7498322 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:7498322 | pubmed:citationSubset | IM | lld:pubmed |
pubmed-article:7498322 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:7498322 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:7498322 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:7498322 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:7498322 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:7498322 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:7498322 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:7498322 | pubmed:status | MEDLINE | lld:pubmed |
pubmed-article:7498322 | pubmed:month | Sep | lld:pubmed |
pubmed-article:7498322 | pubmed:issn | 0014-2999 | lld:pubmed |
pubmed-article:7498322 | pubmed:author | pubmed-author:OhlsteinE HEH | lld:pubmed |
pubmed-article:7498322 | pubmed:author | pubmed-author:EdwardsR MRM | lld:pubmed |
pubmed-article:7498322 | pubmed:author | pubmed-author:BakerEE | lld:pubmed |
pubmed-article:7498322 | pubmed:author | pubmed-author:BrooksD PDP | lld:pubmed |
pubmed-article:7498322 | pubmed:author | pubmed-author:GellaiMM | lld:pubmed |
pubmed-article:7498322 | pubmed:author | pubmed-author:WeinstockJJ | lld:pubmed |
pubmed-article:7498322 | pubmed:author | pubmed-author:AiyarNN | lld:pubmed |
pubmed-article:7498322 | pubmed:author | pubmed-author:WeidleyE FEF | lld:pubmed |
pubmed-article:7498322 | pubmed:author | pubmed-author:FredricksonT... | lld:pubmed |
pubmed-article:7498322 | pubmed:author | pubmed-author:Vickery-Clark... | lld:pubmed |
pubmed-article:7498322 | pubmed:issnType | Print | lld:pubmed |
pubmed-article:7498322 | pubmed:day | 5 | lld:pubmed |
pubmed-article:7498322 | pubmed:volume | 283 | lld:pubmed |
pubmed-article:7498322 | pubmed:owner | NLM | lld:pubmed |
pubmed-article:7498322 | pubmed:authorsComplete | Y | lld:pubmed |
pubmed-article:7498322 | pubmed:pagination | 63-72 | lld:pubmed |
pubmed-article:7498322 | pubmed:dateRevised | 2010-11-18 | lld:pubmed |
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pubmed-article:7498322 | pubmed:year | 1995 | lld:pubmed |
pubmed-article:7498322 | pubmed:articleTitle | Pharmacology of a potent long-acting imidazole-5-acrylic acid angiotensin AT1 receptor antagonist. | lld:pubmed |
pubmed-article:7498322 | pubmed:affiliation | Department of Cardiovascular Pharmacology, SmithKline Beecham Pharmaceuticals, King of Prussia, PA 19406-0939, USA. | lld:pubmed |
pubmed-article:7498322 | pubmed:publicationType | Journal Article | lld:pubmed |