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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
15
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pubmed:dateCreated |
2010-8-5
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pubmed:databankReference |
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pubmed:abstractText |
A series of AMPA receptor positive allosteric modulators has been optimized from poorly penetrant leads to identify molecules with excellent preclinical pharmacokinetics and CNS penetration. These discoveries led to 17i, a potent, efficacious CNS penetrant molecule with an excellent pharmacokinetic profile across preclinical species, which is well tolerated and is also orally bioavailable in humans.
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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 |
1520-4804
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pubmed:author |
pubmed-author:AldegheriLauraL,
pubmed-author:AndreottiDanieleD,
pubmed-author:BallantineStuartS,
pubmed-author:BaxBenjamin DBD,
pubmed-author:HarkerAndy JAJ,
pubmed-author:HarriesMarkM,
pubmed-author:HarrisAndrew JAJ,
pubmed-author:LundJesperJ,
pubmed-author:MelarangeRosemaryR,
pubmed-author:MingardiAnnaA,
pubmed-author:MookherjeeClaudetteC,
pubmed-author:MosleyJulieJ,
pubmed-author:NeveMartaM,
pubmed-author:OliosiBeatriceB,
pubmed-author:ProfetaRobertoR,
pubmed-author:SmithKathrine JKJ,
pubmed-author:SmithPaul WPW,
pubmed-author:SpadaSimoneS,
pubmed-author:ThewlisKevin MKM,
pubmed-author:WardSimon ESE,
pubmed-author:YusafShahnaz PSP
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pubmed:issnType |
Electronic
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pubmed:day |
12
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pubmed:volume |
53
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5801-12
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pubmed:meshHeading |
pubmed-meshheading:20614889-Administration, Oral,
pubmed-meshheading:20614889-Allosteric Regulation,
pubmed-meshheading:20614889-Animals,
pubmed-meshheading:20614889-Biological Availability,
pubmed-meshheading:20614889-Blood Proteins,
pubmed-meshheading:20614889-Blood-Brain Barrier,
pubmed-meshheading:20614889-Callithrix,
pubmed-meshheading:20614889-Cell Line,
pubmed-meshheading:20614889-Crystallography, X-Ray,
pubmed-meshheading:20614889-Dogs,
pubmed-meshheading:20614889-Humans,
pubmed-meshheading:20614889-Indenes,
pubmed-meshheading:20614889-Macaca fascicularis,
pubmed-meshheading:20614889-Male,
pubmed-meshheading:20614889-Microsomes, Liver,
pubmed-meshheading:20614889-Models, Molecular,
pubmed-meshheading:20614889-Protein Binding,
pubmed-meshheading:20614889-Protein Structure, Tertiary,
pubmed-meshheading:20614889-Pyridines,
pubmed-meshheading:20614889-Rats,
pubmed-meshheading:20614889-Rats, Sprague-Dawley,
pubmed-meshheading:20614889-Receptors, AMPA,
pubmed-meshheading:20614889-Species Specificity,
pubmed-meshheading:20614889-Stereoisomerism,
pubmed-meshheading:20614889-Structure-Activity Relationship,
pubmed-meshheading:20614889-Sulfonamides
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pubmed:year |
2010
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pubmed:articleTitle |
Discovery of N-[(2S)-5-(6-fluoro-3-pyridinyl)-2,3-dihydro-1H-inden-2-yl]-2-propanesulfonamide, a novel clinical AMPA receptor positive modulator.
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pubmed:affiliation |
Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Harlow, Essex, UK. simon.e.ward@gsk.com
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pubmed:publicationType |
Journal Article,
Clinical Trial, Phase I
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