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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
4
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pubmed:dateCreated |
2002-2-14
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pubmed:abstractText |
A series of alkylidene hydrazide derivatives containing an alkoxyaryl moiety was optimized. The resulting hydrazide-ethers were competitive antagonists at the human glucagon receptor. Pharmacokinetic experiments showed fast clearance of most of the compounds tested. A representative compound [4-hydroxy-3-cyanobenzoic acid (4-isopropylbenzyloxy-3,5-dimethoxymethylene)hydrazide] with an IC50 value of 20 nM was shown to reduce blood glucose levels in fasted rats.
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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 |
Feb
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:AnderesKennaK,
pubmed-author:BrandChristian LCL,
pubmed-author:GonzalezJavierJ,
pubmed-author:GregorVladV,
pubmed-author:IatsimirskaiaEugeniaE,
pubmed-author:KielDanD,
pubmed-author:KnudsenLotte BLB,
pubmed-author:KukiAtsuoA,
pubmed-author:LakisJamesJ,
pubmed-author:LauJesperJ,
pubmed-author:LingAnthonyA,
pubmed-author:MadsenPeterP,
pubmed-author:MayJohnJ,
pubmed-author:MurphyDougD,
pubmed-author:PleweMichaelM,
pubmed-author:PolinskyAlexA,
pubmed-author:SamsChristian KCK,
pubmed-author:ShiShenghuaS,
pubmed-author:SidelmannUlla GUG,
pubmed-author:TestonKimberlyK,
pubmed-author:TruesdaleLarryL
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pubmed:issnType |
Print
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pubmed:day |
25
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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 |
663-6
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:11844695-Animals,
pubmed-meshheading:11844695-Binding, Competitive,
pubmed-meshheading:11844695-Blood Glucose,
pubmed-meshheading:11844695-Humans,
pubmed-meshheading:11844695-Hydrazines,
pubmed-meshheading:11844695-Hypoglycemic Agents,
pubmed-meshheading:11844695-Inhibitory Concentration 50,
pubmed-meshheading:11844695-Injections,
pubmed-meshheading:11844695-Metabolic Clearance Rate,
pubmed-meshheading:11844695-Microsomes, Liver,
pubmed-meshheading:11844695-Rats,
pubmed-meshheading:11844695-Receptors, Glucagon,
pubmed-meshheading:11844695-Structure-Activity Relationship
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pubmed:year |
2002
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pubmed:articleTitle |
Human glucagon receptor antagonists based on alkylidene hydrazides.
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pubmed:affiliation |
Pfizer Global Research and Development, 10770 Science Center Dr., San Diego, CA 92121, USA. anthony.ling@agouron.com
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pubmed:publicationType |
Journal Article
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