|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
3
|
|
pubmed:dateCreated |
2005-1-24
|
|
pubmed:abstractText |
Starting from a high throughput screening hit, a series of 3,4-dihydro-2H-benzoxazinones has been identified with both high affinity for the 5-HT(1A) receptor and potent 5-HT reuptake inhibitory activity. The 5-(2-methyl)quinolinyloxy derivative combined high 5-HT(1A/1B/1D) receptor affinities with low intrinsic activity and potent inhibition of the 5-HT reuptake site (pK(i)8.2). This compound also had good oral bioavailability and brain penetration in the rat.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Feb
|
|
pubmed:issn |
0960-894X
|
|
pubmed:author |
pubmed-author:AtkinsonPeter JPJ,
pubmed-author:BromidgeSteven MSM,
pubmed-author:DuxonMark SMS,
pubmed-author:GasterLaramie MLM,
pubmed-author:HadleyMichael SMS,
pubmed-author:HammondBeverleyB,
pubmed-author:JohnsonChristopher NCN,
pubmed-author:MiddlemissDerek NDN,
pubmed-author:NorthStephanie ESE,
pubmed-author:PriceGary WGW,
pubmed-author:RamiHarshad KHK,
pubmed-author:RileyGraham JGJ,
pubmed-author:ScottClaire MCM,
pubmed-author:ShawTracey ETE,
pubmed-author:StarrKathryn RKR,
pubmed-author:StempGeoffreyG,
pubmed-author:ThewlisKevin MKM,
pubmed-author:ThomasDavid RDR,
pubmed-author:ThompsonMervynM,
pubmed-author:VongAntonio K KAK,
pubmed-author:WatsonJeannette MJM
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
1
|
|
pubmed:volume |
15
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
737-41
|
|
pubmed:dateRevised |
2010-11-18
|
|
pubmed:meshHeading |
pubmed-meshheading:15664848-Animals,
pubmed-meshheading:15664848-Benzoxazines,
pubmed-meshheading:15664848-Biological Availability,
pubmed-meshheading:15664848-Brain,
pubmed-meshheading:15664848-Cell Line,
pubmed-meshheading:15664848-Drug Stability,
pubmed-meshheading:15664848-Humans,
pubmed-meshheading:15664848-Radioligand Assay,
pubmed-meshheading:15664848-Rats,
pubmed-meshheading:15664848-Serotonin 5-HT1 Receptor Antagonists,
pubmed-meshheading:15664848-Serotonin Uptake Inhibitors,
pubmed-meshheading:15664848-Structure-Activity Relationship,
pubmed-meshheading:15664848-Synaptosomes
|
|
pubmed:year |
2005
|
|
pubmed:articleTitle |
3,4-Dihydro-2H-benzoxazinones are 5-HT(1A) receptor antagonists with potent 5-HT reuptake inhibitory activity.
|
|
pubmed:affiliation |
Psychiatry Center of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK.
|
|
pubmed:publicationType |
Journal Article
|
