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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
21
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pubmed:dateCreated |
2003-10-13
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pubmed:abstractText |
To identify neuroprotective agents after stroke, new substituted tetrahydroquinoline derivatives were designed as antagonists of the glycine binding site associated to the NMDA receptor, satisfying the key pharmacophoric requirements. In particular, the racemate 3c exhibited outstanding in vivo activity in the MCAo model in rats, when given iv both pre- and post-ischemia. Pure enantiomers 3c-(+) and 3c-(-) have been prepared following an original synthetic route. Despite the significant difference of activity observed in vitro, they shown similar neuroprotective profile in the MCAo model in rats.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:AlvaroGiuseppeG,
pubmed-author:ArbanRobertoR,
pubmed-author:BarnabyRobert JRJ,
pubmed-author:BertaniBarbaraB,
pubmed-author:Dal FornoGiovannaG,
pubmed-author:Di FabioRomanoR,
pubmed-author:DonatiDanieleD,
pubmed-author:MesseriTommasoT,
pubmed-author:MicheliFabrizioF,
pubmed-author:PasquarelloAlessandraA,
pubmed-author:PentassugliaGiorgioG,
pubmed-author:PizziMaria DomenicaMD,
pubmed-author:RattiEmiliangeloE,
pubmed-author:ReggianiAngeloA,
pubmed-author:SabbatiniFabioF,
pubmed-author:TranquilliniElviraE
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pubmed:issnType |
Print
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pubmed:day |
3
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pubmed:volume |
13
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3863-6
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pubmed:meshHeading |
pubmed-meshheading:14552796-Animals,
pubmed-meshheading:14552796-Binding Sites,
pubmed-meshheading:14552796-Brain Ischemia,
pubmed-meshheading:14552796-Dose-Response Relationship, Drug,
pubmed-meshheading:14552796-Injections, Intravenous,
pubmed-meshheading:14552796-Middle Cerebral Artery,
pubmed-meshheading:14552796-Molecular Conformation,
pubmed-meshheading:14552796-Neuroprotective Agents,
pubmed-meshheading:14552796-Quinolines,
pubmed-meshheading:14552796-Rats,
pubmed-meshheading:14552796-Receptors, Glycine,
pubmed-meshheading:14552796-Receptors, N-Methyl-D-Aspartate,
pubmed-meshheading:14552796-Stereoisomerism
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pubmed:year |
2003
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pubmed:articleTitle |
Enantiomerically pure tetrahydroquinoline derivatives as in vivo potent antagonists of the glycine binding site associated to the NMDA receptor.
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pubmed:affiliation |
Medicines Research Centre, GlaxoSmithKline S.p.A, Via Fleming 4, 37135 Verona, Italy. rdf26781@gsk.com
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pubmed:publicationType |
Journal Article
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