rdf:type |
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lifeskim:mentions |
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pubmed:issue |
5
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pubmed:dateCreated |
2005-3-3
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pubmed:abstractText |
Indolic N-benzylation of naltrindole reportedly extends the duration of delta-opioid receptor (DOR) antagonism. Similar modification of the kappa-opioid receptor (KOR) antagonist norBNI (1a) and its 17,17'-diNMe analogue (1d), a low potency mu-opioid receptor (MOR) partial agonist, was found to affect predominantly their MOR activity. When administered systemically in mouse antinociceptive assays, N-benzyl-norBNI (1b) had only MOR agonist activity of relatively short duration whereas on central administration it had only a KOR-antagonist action of extremely long duration.
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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 |
http://linkedlifedata.com/resource/pubmed/chemical/Analgesics,
http://linkedlifedata.com/resource/pubmed/chemical/Guanosine 5'-O-(3-Thiotriphosphate),
http://linkedlifedata.com/resource/pubmed/chemical/Naltrexone,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrroles,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, delta,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, kappa,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, mu,
http://linkedlifedata.com/resource/pubmed/chemical/norbinaltorphimine
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0022-2623
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pubmed:author |
|
pubmed:issnType |
Print
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pubmed:day |
10
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pubmed:volume |
48
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1676-9
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:15743210-Analgesics,
pubmed-meshheading:15743210-Animals,
pubmed-meshheading:15743210-Cell Line,
pubmed-meshheading:15743210-Guanosine 5'-O-(3-Thiotriphosphate),
pubmed-meshheading:15743210-Humans,
pubmed-meshheading:15743210-Mice,
pubmed-meshheading:15743210-Naltrexone,
pubmed-meshheading:15743210-Pyrroles,
pubmed-meshheading:15743210-Radioligand Assay,
pubmed-meshheading:15743210-Receptors, Opioid, delta,
pubmed-meshheading:15743210-Receptors, Opioid, kappa,
pubmed-meshheading:15743210-Receptors, Opioid, mu,
pubmed-meshheading:15743210-Structure-Activity Relationship
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pubmed:year |
2005
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pubmed:articleTitle |
Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist.
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pubmed:affiliation |
Department of Pharmacy and Pharmacology, University of Bath, Bath BA2 7AY, UK.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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