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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
5
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pubmed:dateCreated |
2003-2-20
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pubmed:abstractText |
To investigate the anorectic potential of NPY5 receptor antagonists, we have profiled the in vitro and in vivo properties of 3-[2-[6-(2-tert-butoxyethoxy)pyridin-3-yl]-1H-imidazol-4-yl]benzonitrile hydrochloride salt (1). This compound was found to have excellent NPY5 receptor affinity and selectivity, potent functional antagonism, and good peripheral and central nervous system exposure in rats. This compound attenuated bovine pancreatic polypeptide induced food intake in rats but failed to demonstrate anorectic activity in rodent natural feeding models.
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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:CassellaJames VJV,
pubmed-author:DaSilva-JardinePaul APA,
pubmed-author:ElliottRichard LRL,
pubmed-author:HammondMarlysM,
pubmed-author:HargroveDiane MDM,
pubmed-author:KalvassJ CoryJC,
pubmed-author:MackChristine MCM,
pubmed-author:MartinKelly AKA,
pubmed-author:MaurerTristan STS,
pubmed-author:MorganBradley PBP,
pubmed-author:OliverRobert MRM,
pubmed-author:PattersonTerrell ATA,
pubmed-author:StevensonRalph WRW,
pubmed-author:UriAA
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pubmed:issnType |
Print
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pubmed:day |
27
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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 |
670-3
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:12593645-Animals,
pubmed-meshheading:12593645-Brain,
pubmed-meshheading:12593645-Calcium,
pubmed-meshheading:12593645-Cattle,
pubmed-meshheading:12593645-Cerebrospinal Fluid,
pubmed-meshheading:12593645-Eating,
pubmed-meshheading:12593645-Humans,
pubmed-meshheading:12593645-Imidazoles,
pubmed-meshheading:12593645-Male,
pubmed-meshheading:12593645-Nitriles,
pubmed-meshheading:12593645-Pancreatic Polypeptide,
pubmed-meshheading:12593645-Rats,
pubmed-meshheading:12593645-Rats, Sprague-Dawley,
pubmed-meshheading:12593645-Rats, Wistar,
pubmed-meshheading:12593645-Receptors, Neuropeptide Y,
pubmed-meshheading:12593645-Tissue Distribution,
pubmed-meshheading:12593645-Tumor Cells, Cultured
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pubmed:year |
2003
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pubmed:articleTitle |
In vitro and in vivo characterization of 3-[2-[6-(2-tert-butoxyethoxy)pyridin-3-yl]-1H-imidazol-4-yl]benzonitrile hydrochloride salt, a potent and selective NPY5 receptor antagonist.
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pubmed:affiliation |
Cardiovascular and Metabolic Diseases, PGRD, Pfizer Inc., Groton, Connecticut 06340, and Neurogen Corporation, Branford, Connecticut 06405, USA. richard_l_elliot@groton.pfizer.com
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pubmed:publicationType |
Journal Article,
In Vitro
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