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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
2
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pubmed:dateCreated |
2003-1-9
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pubmed:abstractText |
New 3-aryl-6-(3-thienyl)pyrazolo[1,5-a]pyrimidin-7-ones (2a-j) are synthesized and evaluated in vitro on Bz/GABA(A) receptors and on recombinant benzodiazepine receptors (alpha x beta 2/3 gamma 2; x = 1-3, 5) expressed in HEK293 cells. SAR studies on the new compounds are conducted and molecular modeling is accomplished to better investigate requirements leading to subtype selectivity. Some of the synthesized compounds are tested in vivo to explore their pharmacological effect as a consequence of their high alpha 1 beta 2 gamma 2 subtype selectivity observed in vitro.
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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 |
Jan
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:BesnardFrançoisF,
pubmed-author:BonacciniClaudiaC,
pubmed-author:BruniFabrizioF,
pubmed-author:CicianiGiovannaG,
pubmed-author:CostaBarbaraB,
pubmed-author:CostagliCamillaC,
pubmed-author:CostanzoAnnarellaA,
pubmed-author:GratteriPaolaP,
pubmed-author:GuerriniGabriellaG,
pubmed-author:Malmberg AielloPetraP,
pubmed-author:MartiniClaudiaC,
pubmed-author:RenardStephaneS,
pubmed-author:SelleriSilviaS
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pubmed:issnType |
Print
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pubmed:day |
16
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pubmed:volume |
46
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
310-3
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:12519068-Animals,
pubmed-meshheading:12519068-Anti-Anxiety Agents,
pubmed-meshheading:12519068-Anticonvulsants,
pubmed-meshheading:12519068-Binding, Competitive,
pubmed-meshheading:12519068-Brain,
pubmed-meshheading:12519068-Cattle,
pubmed-meshheading:12519068-Ligands,
pubmed-meshheading:12519068-Models, Molecular,
pubmed-meshheading:12519068-Muscle Relaxants, Central,
pubmed-meshheading:12519068-Pyrimidines,
pubmed-meshheading:12519068-Quantitative Structure-Activity Relationship,
pubmed-meshheading:12519068-Receptors, GABA-A
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pubmed:year |
2003
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pubmed:articleTitle |
Synthesis and benzodiazepine receptor affinity of pyrazolo[1,5-a]pyrimidine derivatives. 3. New 6-(3-thienyl) series as alpha 1 selective ligands.
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pubmed:affiliation |
Department of Pharmaceutical Sciences, University of Firenze, Via G. Capponi 9, 50121 Firenze, Italy. silvia.selleri@unifi.it
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pubmed:publicationType |
Journal Article,
In Vitro
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