Source:http://linkedlifedata.com/resource/pubmed/id/14505681
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
20
|
| pubmed:dateCreated |
2003-9-24
|
| pubmed:abstractText |
A series of 4-(2-pyridyl)piperazine-1-carboxamide analogues based on the lead compound 1 was synthesized and evaluated for VR1 antagonist activity in capsaicin-induced (CAP) and pH (5.5)-induced (pH) FLIPR assays in a rat VR1-expressing HEK293 cell line. Potent VR1 antagonists were identified through SAR studies. From these studies, 18 was found to be very potent in the in vitro assay [IC(50)=4.8 nM (pH) and 35 nM (CAP)] and orally available in rat (F%=15.1).
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Oct
|
| pubmed:issn |
0960-894X
|
| pubmed:author |
pubmed-author:HachichaMohamedM,
pubmed-author:IslamKhondakerK,
pubmed-author:KyleDonald JDJ,
pubmed-author:PatelAniketA,
pubmed-author:RotshteynYakovY,
pubmed-author:SchmidLori ALA,
pubmed-author:SunQunQ,
pubmed-author:TafesseLaykeaL,
pubmed-author:ValenzanoKenneth JKJ,
pubmed-author:VictorySam FSF,
pubmed-author:ZhangChongwuC,
pubmed-author:ZhouXiaomingX
|
| pubmed:issnType |
Print
|
| pubmed:day |
20
|
| pubmed:volume |
13
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
3611-6
|
| pubmed:dateRevised |
2005-11-17
|
| pubmed:meshHeading | |
| pubmed:year |
2003
|
| pubmed:articleTitle |
4-(2-pyridyl)piperazine-1-carboxamides: potent vanilloid receptor 1 antagonists.
|
| pubmed:affiliation |
Purdue Pharma L.P., 6 Cedar Brook Drive, Cranbury, NJ 08512, USA. qun.sun@pharma.com
|
| pubmed:publicationType |
Journal Article
|