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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
16
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pubmed:dateCreated |
2002-7-25
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pubmed:abstractText |
A library of compounds biased toward opioid receptor antagonist activity was prepared by incorporating N-phenylpropyl-4beta-methyl-5-(3-hydroxyphenyl)morphans as the core scaffold using simultaneous solution phase synthetic methodology. From this library, N-phenylpropyl-4beta-methyl-5-(3-hydroxyphenyl)-7alpha-[3-(1-piperidinyl)propanamido]morphan [(-)-3b] was identified as the first potent and selective kappa opioid receptor antagonist from the 5-phenylmorphan class of opioids.
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pubmed:grant |
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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 |
Aug
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pubmed:issn |
0022-2623
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pubmed:author |
pubmed-author:AtkinsonRobert NRN,
pubmed-author:BurgessJason PJP,
pubmed-author:CantrellBuddy EBE,
pubmed-author:CarrollF IvyFI,
pubmed-author:DerschChristina MCM,
pubmed-author:FixScott ESE,
pubmed-author:GigstadKenneth MKM,
pubmed-author:MascarellaS WayneSW,
pubmed-author:NamdevNiveditaN,
pubmed-author:RothmanRichard BRB,
pubmed-author:ThomasJames BJB,
pubmed-author:VinsonN ArianeNA,
pubmed-author:XuHengH,
pubmed-author:ZimmermanDennis MDM
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pubmed:issnType |
Print
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pubmed:day |
1
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pubmed:volume |
45
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3524-30
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:12139463-Animals,
pubmed-meshheading:12139463-Bicyclo Compounds, Heterocyclic,
pubmed-meshheading:12139463-Brain,
pubmed-meshheading:12139463-CHO Cells,
pubmed-meshheading:12139463-Combinatorial Chemistry Techniques,
pubmed-meshheading:12139463-Cricetinae,
pubmed-meshheading:12139463-Guinea Pigs,
pubmed-meshheading:12139463-Humans,
pubmed-meshheading:12139463-Ligands,
pubmed-meshheading:12139463-Morphinans,
pubmed-meshheading:12139463-Radioligand Assay,
pubmed-meshheading:12139463-Rats,
pubmed-meshheading:12139463-Receptors, Opioid, kappa,
pubmed-meshheading:12139463-Stereoisomerism,
pubmed-meshheading:12139463-Structure-Activity Relationship
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pubmed:year |
2002
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pubmed:articleTitle |
Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans.
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pubmed:affiliation |
Chemistry and Life Sciences, Research Triangle Institute, Research Triangle Park, NC 27709, USA.
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, U.S. Gov't, P.H.S.
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