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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
3
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pubmed:dateCreated |
2008-2-7
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pubmed:abstractText |
Ghrelin receptor ligands based on trisubstituted 1,2,4-triazole structure were synthesized and evaluated for their in vitro binding and biological activity. In this study, we explored the replacement of the alpha-aminoisobutyryl moiety by aromatic or heteroaromatic groups. Compounds 5 and 34 acted as potent in vivo antagonists of hexarelin-stimulated food intake. These two compounds did not stimulate growth hormone secretion in rodents and did not antagonize growth hormone secretion induced by hexarelin.
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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 |
0022-2623
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pubmed:author |
pubmed-author:BergéGilbertG,
pubmed-author:DemangeLucL,
pubmed-author:FehrentzJean-AlainJA,
pubmed-author:GagneDidierD,
pubmed-author:GalleyrandJean-ClaudeJC,
pubmed-author:KtenidesM AMA,
pubmed-author:LocatelliVittorioV,
pubmed-author:MartinezJeanJ,
pubmed-author:MoulinAlineA,
pubmed-author:MousseauxDelphineD,
pubmed-author:RyanJoanneJ,
pubmed-author:SanchezPierreP,
pubmed-author:TorselloAntonioA
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pubmed:issnType |
Print
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pubmed:day |
14
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pubmed:volume |
51
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
689-93
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pubmed:meshHeading |
pubmed-meshheading:18193826-Animals,
pubmed-meshheading:18193826-Anti-Obesity Agents,
pubmed-meshheading:18193826-Eating,
pubmed-meshheading:18193826-Growth Hormone,
pubmed-meshheading:18193826-Humans,
pubmed-meshheading:18193826-LLC-PK1 Cells,
pubmed-meshheading:18193826-Oligopeptides,
pubmed-meshheading:18193826-Picolines,
pubmed-meshheading:18193826-Pyrazines,
pubmed-meshheading:18193826-Radioligand Assay,
pubmed-meshheading:18193826-Rats,
pubmed-meshheading:18193826-Receptors, Ghrelin,
pubmed-meshheading:18193826-Stereoisomerism,
pubmed-meshheading:18193826-Structure-Activity Relationship,
pubmed-meshheading:18193826-Swine,
pubmed-meshheading:18193826-Triazoles
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pubmed:year |
2008
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pubmed:articleTitle |
New trisubstituted 1,2,4-triazole derivatives as potent ghrelin receptor antagonists. 3. Synthesis and pharmacological in vitro and in vivo evaluations.
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pubmed:affiliation |
Institut des Biomolécules Max Mousseron, UMR 5247, CNRS, Universités Montpellier 1, Montpellier 2, Montpellier Cedex 5, France.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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