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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
10
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pubmed:dateCreated |
2004-4-27
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pubmed:abstractText |
We have identified and synthesized a series of [1,2,4]triazolo[3,4-a]phthalazine derivatives as high-affinity ligands to alpha 2 delta-1 subunit of voltage gated calcium channels. Structure-activity relationship studies directed toward improving the potency and physical properties of 2 lead to the discovery of 20 (IC(50)=15 nM) and (S)-22 (IC(50)=30 nM). A potent and selective radioligand, [(3)H]-(S)-22 was also synthesized to demonstrate that this ligand binds to the same site as gabapentin.
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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 |
May
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:AiyarJayashreeJ,
pubmed-author:BezverkovRobertR,
pubmed-author:GunznerJanetJ,
pubmed-author:LebsackAlec DAD,
pubmed-author:LiuWenshengW,
pubmed-author:MunozBenitoB,
pubmed-author:PracittoRichardR,
pubmed-author:SantiniAngelinaA,
pubmed-author:SchaffhauserHervéH,
pubmed-author:VenkatramanShankarS,
pubmed-author:WangBoweiB
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pubmed:issnType |
Print
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pubmed:day |
17
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pubmed:volume |
14
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2463-7
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pubmed:meshHeading |
pubmed-meshheading:15109633-Amines,
pubmed-meshheading:15109633-Analgesics,
pubmed-meshheading:15109633-Binding Sites,
pubmed-meshheading:15109633-Calcium Channel Blockers,
pubmed-meshheading:15109633-Calcium Channels,
pubmed-meshheading:15109633-Cyclohexanecarboxylic Acids,
pubmed-meshheading:15109633-Humans,
pubmed-meshheading:15109633-Inhibitory Concentration 50,
pubmed-meshheading:15109633-Ligands,
pubmed-meshheading:15109633-Phthalazines,
pubmed-meshheading:15109633-Radioligand Assay,
pubmed-meshheading:15109633-Structure-Activity Relationship,
pubmed-meshheading:15109633-gamma-Aminobutyric Acid
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pubmed:year |
2004
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pubmed:articleTitle |
Identification and synthesis of [1,2,4]triazolo[3,4-a]phthalazine derivatives as high-affinity ligands to the alpha 2 delta-1 subunit of voltage gated calcium channel.
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pubmed:affiliation |
Department of Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, San Diego, CA 92121, USA. alec_lebsack@merck.com
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pubmed:publicationType |
Journal Article
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