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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
8
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pubmed:dateCreated |
2003-4-3
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pubmed:abstractText |
The 14-amino analogue of oxymorphindole (OMI) was synthesized and found to possess delta-opioid binding affinity and selectivity similar to OMI. Substitution of the amino group with alkyl, arylalkyl, and acyl groups had relatively little effect on delta-affinity but delta-selectivity was reduced. In functional assays the 14-phenylacetylamino derivative 6d was a selective delta-agonist whereas the phenethylamino analogue 5d was a mu-agonist and low efficacy delta partial agonist that warrants further investigation as an analgesic with low tolerance and dependence.
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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 |
Apr
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
10
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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 |
1563-6
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:12672258-Analgesics, Opioid,
pubmed-meshheading:12672258-Animals,
pubmed-meshheading:12672258-Binding, Competitive,
pubmed-meshheading:12672258-CHO Cells,
pubmed-meshheading:12672258-Cricetinae,
pubmed-meshheading:12672258-Morpholines,
pubmed-meshheading:12672258-Radioligand Assay,
pubmed-meshheading:12672258-Receptors, Opioid, delta,
pubmed-meshheading:12672258-Receptors, Opioid, mu,
pubmed-meshheading:12672258-Structure-Activity Relationship
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pubmed:year |
2003
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pubmed:articleTitle |
14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
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pubmed:affiliation |
Department of Pharmacy and Pharmacology, University of Bath, UK.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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