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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
20
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pubmed:dateCreated |
2002-9-24
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pubmed:abstractText |
A series of 7-substituted-3-cyclobutylamino-4H-1,2,4-benzothiadiazine-1,1-dioxide derivatives has been synthesized and evaluated as K(ATP) channel agonists using the inside-out excised patch clamp technique. The most active compounds were approximately 20-fold more potent than diazoxide in opening K(ATP) channels. A linear relationship exists between the potency of the compound and the sigma value of the 7-substituent with electron-withdrawing groups exhibiting higher activity. These compounds may be useful in modulating insulin release from pancreatic beta-cells and in diseases associated with hyperinsulinemia.
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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 |
Oct
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:AllenScott HSH,
pubmed-author:GarridoDulceD,
pubmed-author:MertzRobert JRJ,
pubmed-author:PeatAndrew JAJ,
pubmed-author:PfohlJeffrey LJL,
pubmed-author:TerryChristopher MCM,
pubmed-author:ThomsonStephen ASA,
pubmed-author:TownsendClaireC,
pubmed-author:TruaxJim FJF,
pubmed-author:VeaseyRobert LRL,
pubmed-author:WorleyJennings FJF3rd
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pubmed:issnType |
Print
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pubmed:day |
21
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pubmed:volume |
12
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2977-80
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pubmed:dateRevised |
2011-11-17
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pubmed:meshHeading |
pubmed-meshheading:12270187-ATP-Binding Cassette Transporters,
pubmed-meshheading:12270187-Benzothiadiazines,
pubmed-meshheading:12270187-Electrons,
pubmed-meshheading:12270187-Electrophysiology,
pubmed-meshheading:12270187-Humans,
pubmed-meshheading:12270187-Insulin,
pubmed-meshheading:12270187-KATP Channels,
pubmed-meshheading:12270187-Lymphocytes,
pubmed-meshheading:12270187-Patch-Clamp Techniques,
pubmed-meshheading:12270187-Potassium Channels,
pubmed-meshheading:12270187-Potassium Channels, Inwardly Rectifying,
pubmed-meshheading:12270187-Protons,
pubmed-meshheading:12270187-Spectrophotometry, Ultraviolet,
pubmed-meshheading:12270187-Structure-Activity Relationship
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pubmed:year |
2002
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pubmed:articleTitle |
Synthesis and evaluation of 7-substituted-3-cyclobutylamino-4H-1,2,4-benzothiadiazine-1,1-dioxide derivatives as K(ATP) channel agonists.
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pubmed:affiliation |
GlaxoSmithKline Research and Development, 5Moore Drive, Research Triangle Park, NC 27709, USA. ajp25551@gsk.com
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pubmed:publicationType |
Journal Article
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