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rdf:type |
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lifeskim:mentions |
umls-concept:C0003469,
umls-concept:C0005456,
umls-concept:C0016904,
umls-concept:C0034289,
umls-concept:C0087111,
umls-concept:C0205531,
umls-concept:C0226896,
umls-concept:C0243192,
umls-concept:C0442027,
umls-concept:C0935763,
umls-concept:C1527415,
umls-concept:C1879648
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pubmed:issue |
1
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pubmed:dateCreated |
2006-1-5
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|
pubmed:abstractText |
A series of high-affinity GABA(A) agonists with good oral bioavailability in rat and dog and functional selectivity for the GABA(A)alpha2 and -alpha3 subtypes is reported. The 7-trifluoromethylimidazopyrimidine 14g and the 7-propan-2-olimidazopyrimidine 14k are anxiolytic in both conditioned and unconditioned animal models of anxiety with minimal sedation observed at full BZ binding site occupancy.
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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 |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Jan
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|
pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:AtackJohn RJR,
pubmed-author:BlackabyWesley PWP,
pubmed-author:BrownNicolaN,
pubmed-author:CastroJosé LJL,
pubmed-author:CookSusan MSM,
pubmed-author:CrawforthJames MJM,
pubmed-author:FerrisPushpinderP,
pubmed-author:GoodacreSimon CSC,
pubmed-author:HallettDavid JDJ,
pubmed-author:KellySarahS,
pubmed-author:LewisRichard TRT,
pubmed-author:MarshallGeorgeG,
pubmed-author:OwensAndrew PAP,
pubmed-author:PikeAndrewA,
pubmed-author:SmithAlison JAJ,
pubmed-author:SohalBindiB,
pubmed-author:StanleyJoannaJ,
pubmed-author:StreetLeslie JLJ,
pubmed-author:WaffordKeith AKA
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pubmed:issnType |
Print
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pubmed:day |
12
|
|
pubmed:volume |
49
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
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pubmed:pagination |
35-8
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pubmed:dateRevised |
2011-11-17
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pubmed:meshHeading |
pubmed-meshheading:16392789-Administration, Oral,
pubmed-meshheading:16392789-Animals,
pubmed-meshheading:16392789-Anxiety Disorders,
pubmed-meshheading:16392789-Binding Sites,
pubmed-meshheading:16392789-Biological Availability,
pubmed-meshheading:16392789-Cell Line,
pubmed-meshheading:16392789-Disease Models, Animal,
pubmed-meshheading:16392789-Dogs,
pubmed-meshheading:16392789-Dose-Response Relationship, Drug,
pubmed-meshheading:16392789-Drug Evaluation, Preclinical,
pubmed-meshheading:16392789-GABA-A Receptor Agonists,
pubmed-meshheading:16392789-Humans,
pubmed-meshheading:16392789-Molecular Structure,
pubmed-meshheading:16392789-Patch-Clamp Techniques,
pubmed-meshheading:16392789-Pyrimidines,
pubmed-meshheading:16392789-Rats,
pubmed-meshheading:16392789-Receptors, GABA-A,
pubmed-meshheading:16392789-Structure-Activity Relationship
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pubmed:year |
2006
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pubmed:articleTitle |
Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck Sharp Laboratory, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex, UK.
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pubmed:publicationType |
Journal Article
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