Source:http://linkedlifedata.com/resource/pubmed/id/14711299
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
2004-1-8
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pubmed:abstractText |
A structurally novel opioid delta receptor selective antagonist has been identified. This compound, (+)-5-(3-hydroxyphenyl)-4-methyl-2-(3-phenylpropyl)-2-azabicyclo[3.3.1]non-7-yl-(1-phenyl-1-cyclopentane)carboxamide [(+)-KF4, (+)-4], showed a K(e) value of 0.15 nM in the [(35)S]GTPgammaS functional assay. (+)-KF4 is also a delta inverse agonist with an IC(50) value of 1.8 nM. To our knowledge, this is the first potent and selective delta opioid receptor antagonist from the 5-phenylmorphan class of opioids.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
47
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
281-4
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:14711299-Animals,
pubmed-meshheading:14711299-Bicyclo Compounds, Heterocyclic,
pubmed-meshheading:14711299-Binding, Competitive,
pubmed-meshheading:14711299-CHO Cells,
pubmed-meshheading:14711299-Cricetinae,
pubmed-meshheading:14711299-Humans,
pubmed-meshheading:14711299-Radioligand Assay,
pubmed-meshheading:14711299-Receptors, Opioid, delta,
pubmed-meshheading:14711299-Structure-Activity Relationship
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pubmed:year |
2004
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pubmed:articleTitle |
Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity.
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pubmed:affiliation |
Chemistry and Life Sciences, Research Triangle Institute, Research Triangle Park, North Carolina 27709, USA. fic@rti.org
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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