Source:http://linkedlifedata.com/resource/pubmed/id/15027853
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
7
|
| pubmed:dateCreated |
2004-3-18
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| pubmed:abstractText |
Introduction of nitrogen-containing heteroaromatic groups at the 4-position of the quinoline moiety of our non-peptide B(2) receptor antagonists resulted in enhancing binding affinities for the human B(2) receptor and reducing binding affinities for the guinea pig one, providing new structural insights into species difference. A CoMFA study focused on the diversity of the quinoline moiety afforded correlative and predictive QSAR models of binding for the human B(2) receptor but not for the guinea pig one. A series of 4-(1-imidazolyl)quinoline derivatives could be dissolved in a 5% aqueous solution of citric acid up to a concentration of 10 mg/mL. A representative compound 48a inhibited the specific binding of [(3)H]BK to the cloned human B(2) receptor expressed in Chinese hamster ovary cells with an IC(50) value of 0.26 nM and significantly inhibited BK-induced bronchoconstriction in guinea pigs even at 1 microg/kg by intravenous administration.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Mar
|
| pubmed:issn |
0022-2623
|
| pubmed:author |
pubmed-author:AbeYoshitoY,
pubmed-author:AramoriIchiroI,
pubmed-author:AsanoMasayukiM,
pubmed-author:HatoriChieC,
pubmed-author:ImaiKeisukeK,
pubmed-author:InamuraNoriakiN,
pubmed-author:KatayamaAkiraA,
pubmed-author:KayakiriHiroshiH,
pubmed-author:MizutaniTsuyoshiT,
pubmed-author:OkuTeruoT,
pubmed-author:SawadaYukiY,
pubmed-author:TanakaHirokazuH
|
| pubmed:issnType |
Print
|
| pubmed:day |
25
|
| pubmed:volume |
47
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
1617-30
|
| pubmed:dateRevised |
2006-11-15
|
| pubmed:meshHeading |
pubmed-meshheading:15027853-Animals,
pubmed-meshheading:15027853-Bronchoconstriction,
pubmed-meshheading:15027853-CHO Cells,
pubmed-meshheading:15027853-Cricetinae,
pubmed-meshheading:15027853-Guinea Pigs,
pubmed-meshheading:15027853-Humans,
pubmed-meshheading:15027853-Ileum,
pubmed-meshheading:15027853-Imidazoles,
pubmed-meshheading:15027853-Male,
pubmed-meshheading:15027853-Models, Molecular,
pubmed-meshheading:15027853-Quantitative Structure-Activity Relationship,
pubmed-meshheading:15027853-Quinolines,
pubmed-meshheading:15027853-Radioligand Assay,
pubmed-meshheading:15027853-Rats,
pubmed-meshheading:15027853-Rats, Inbred Lew,
pubmed-meshheading:15027853-Receptor, Bradykinin B2,
pubmed-meshheading:15027853-Solubility,
pubmed-meshheading:15027853-Species Specificity,
pubmed-meshheading:15027853-Water
|
| pubmed:year |
2004
|
| pubmed:articleTitle |
A new series of highly potent non-peptide bradykinin B2 receptor antagonists incorporating the 4-heteroarylquinoline framework. Improvement of aqueous solubility and new insights into species difference.
|
| pubmed:affiliation |
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co. Ltd., 5-2-3 Tokodai, Tsukuba, Ibaraki 300-2698, Japan.
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| pubmed:publicationType |
Journal Article,
In Vitro
|