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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
8
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pubmed:dateCreated |
2000-12-27
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pubmed:abstractText |
Water soluble 8-methylureido-10-amino-10-methyl-imidazo[1,2-a]indeno[1,2-e]pyraz ine-4-one 4 represents a novel class of highly potent and selective AMPA receptors antagonists with in vivo activity. The dextrorotatory isomer (+)-4 was found to display the highest affinity with an IC50 of 10 nM. It also exhibited very good anticonvulsant effects after i.p., s.c. and i.v. administration in mice subjected to electrical convulsions (MES) and i.p. in audiogenic seizure-e in DBA/2 mice (ED50's < or = 10 mg/kg).
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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 |
Aug
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pubmed:issn |
0968-0896
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pubmed:author |
pubmed-author:BohmeG AGA,
pubmed-author:BoireauAA,
pubmed-author:ChevéMM,
pubmed-author:DamourDD,
pubmed-author:DebonoM WMW,
pubmed-author:Genevois-BorellaAA,
pubmed-author:ImperatoAA,
pubmed-author:JimonetPP,
pubmed-author:MignaniSS,
pubmed-author:PrattJJ,
pubmed-author:RandleJ CJC,
pubmed-author:RibeillYY,
pubmed-author:StutzmannJ MJM,
pubmed-author:VuilhorgneMM
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pubmed:issnType |
Print
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pubmed:volume |
8
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2211-7
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:11003165-Animals,
pubmed-meshheading:11003165-Anticonvulsants,
pubmed-meshheading:11003165-Brain Chemistry,
pubmed-meshheading:11003165-Cerebral Cortex,
pubmed-meshheading:11003165-Imidazoles,
pubmed-meshheading:11003165-Kainic Acid,
pubmed-meshheading:11003165-Male,
pubmed-meshheading:11003165-Mice,
pubmed-meshheading:11003165-Microinjections,
pubmed-meshheading:11003165-Molecular Structure,
pubmed-meshheading:11003165-Oocytes,
pubmed-meshheading:11003165-Patch-Clamp Techniques,
pubmed-meshheading:11003165-Pyrazines,
pubmed-meshheading:11003165-RNA, Messenger,
pubmed-meshheading:11003165-Radioligand Assay,
pubmed-meshheading:11003165-Rats,
pubmed-meshheading:11003165-Receptors, AMPA,
pubmed-meshheading:11003165-Stereoisomerism,
pubmed-meshheading:11003165-alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid
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pubmed:year |
2000
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pubmed:articleTitle |
8-Methylureido-10-amino-10-methyl-imidazo[1,2-a]indeno[1,2-e] pyrazine-4-ones: highly in vivo potent and selective AMPA receptor antagonists.
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pubmed:affiliation |
Aventis Pharma S.A., Centre de Recherche de Vitry-Alfortville, Vitry-sur-Seine, France.
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pubmed:publicationType |
Journal Article
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