rdf:type |
|
lifeskim:mentions |
umls-concept:C0020792,
umls-concept:C0205314,
umls-concept:C0205531,
umls-concept:C0226896,
umls-concept:C0442027,
umls-concept:C0679622,
umls-concept:C0935763,
umls-concept:C1415306,
umls-concept:C1446409,
umls-concept:C1527415,
umls-concept:C1709060
|
pubmed:issue |
2
|
pubmed:dateCreated |
2010-2-3
|
pubmed:abstractText |
The optimisation of an HTS hit series (1) leading to the identification of structurally novel, selective, orally bioavailable mGluR2 positive modulators GSK1331258 and GSK1331268 is described. Structure-activity relationships, attenuation of dopaminergic activity, and potentiation of mGluR2 responses in rat hippocampal MPP-DG synapses are also reported.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Jan
|
pubmed:issn |
1464-3405
|
pubmed:author |
pubmed-author:ADLEE HEH,
pubmed-author:BianchiFedericaF,
pubmed-author:BranchCliveC,
pubmed-author:CortiCorradoC,
pubmed-author:D'AlessandroPier LPL,
pubmed-author:GarlandStephen LSL,
pubmed-author:KoppeEmma LEL,
pubmed-author:MontanariDinoD,
pubmed-author:NashDavidD,
pubmed-author:OsborneGregG,
pubmed-author:PerezPalomaP,
pubmed-author:PowneyBenB,
pubmed-author:RochevilleMagalieM,
pubmed-author:RothAdelheidA,
pubmed-author:SavaAnnaA,
pubmed-author:SmithPaul WPW,
pubmed-author:UgoliniAnnarosaA,
pubmed-author:WatsonStephen PSP,
pubmed-author:de la FuenteJesúsJ
|
pubmed:copyrightInfo |
Copyright 2009 Elsevier Ltd. All rights reserved.
|
pubmed:issnType |
Electronic
|
pubmed:day |
15
|
pubmed:volume |
20
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
759-62
|
pubmed:meshHeading |
pubmed-meshheading:20005096-Administration, Oral,
pubmed-meshheading:20005096-Allosteric Regulation,
pubmed-meshheading:20005096-Animals,
pubmed-meshheading:20005096-Benzimidazoles,
pubmed-meshheading:20005096-Dopamine,
pubmed-meshheading:20005096-High-Throughput Screening Assays,
pubmed-meshheading:20005096-Piperazines,
pubmed-meshheading:20005096-Rats,
pubmed-meshheading:20005096-Receptors, Metabotropic Glutamate,
pubmed-meshheading:20005096-Structure-Activity Relationship,
pubmed-meshheading:20005096-Synaptic Potentials
|
pubmed:year |
2010
|
pubmed:articleTitle |
The identification of structurally novel, selective, orally bioavailable positive modulators of mGluR2.
|
pubmed:affiliation |
GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, New Frontiers Science Park, Harlow, UK.
|
pubmed:publicationType |
Journal Article
|