rdf:type |
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lifeskim:mentions |
umls-concept:C0068389,
umls-concept:C0205549,
umls-concept:C0221874,
umls-concept:C0243076,
umls-concept:C0439849,
umls-concept:C0445223,
umls-concept:C0991876,
umls-concept:C1280500,
umls-concept:C1552599,
umls-concept:C1704737,
umls-concept:C1704787
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pubmed:issue |
20
|
pubmed:dateCreated |
2001-2-20
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pubmed:abstractText |
The study of kappa-opioid receptor function in vivo has been hampered by the limited choice of selective kappa-antagonists. Recently discovered kappa-antagonists have not yet been utilised in vivo. We here report the synthesis and in vitro evaluation of a new amidine derivative of naltrindole. It showed substantially greater kappa-selectivity in binding assays than known analogues with shorter spacer in the amidine side chain. This indicates that in nor-BNI and related selective kappa-antagonists, the second basic centre may not be ideally located.
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pubmed:grant |
|
pubmed:language |
eng
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pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Amidines,
http://linkedlifedata.com/resource/pubmed/chemical/Benzeneacetamides,
http://linkedlifedata.com/resource/pubmed/chemical/Enkephalin, Ala(2)-MePhe(4)-Gly(5)-,
http://linkedlifedata.com/resource/pubmed/chemical/Enkephalin, D-Penicillamine (2,5)-,
http://linkedlifedata.com/resource/pubmed/chemical/Indicators and Reagents,
http://linkedlifedata.com/resource/pubmed/chemical/Naltrexone,
http://linkedlifedata.com/resource/pubmed/chemical/Narcotic Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Pyrrolidines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, kappa,
http://linkedlifedata.com/resource/pubmed/chemical/U 69593,
http://linkedlifedata.com/resource/pubmed/chemical/naltrindole
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pubmed:status |
MEDLINE
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pubmed:month |
Oct
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pubmed:issn |
0960-894X
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pubmed:author |
|
pubmed:issnType |
Print
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pubmed:day |
16
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pubmed:volume |
10
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2259-61
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:11055333-Amidines,
pubmed-meshheading:11055333-Animals,
pubmed-meshheading:11055333-Benzeneacetamides,
pubmed-meshheading:11055333-Binding, Competitive,
pubmed-meshheading:11055333-Brain,
pubmed-meshheading:11055333-Cell Membrane,
pubmed-meshheading:11055333-Drug Design,
pubmed-meshheading:11055333-Enkephalin, Ala(2)-MePhe(4)-Gly(5)-,
pubmed-meshheading:11055333-Enkephalin, D-Penicillamine (2,5)-,
pubmed-meshheading:11055333-Guinea Pigs,
pubmed-meshheading:11055333-Indicators and Reagents,
pubmed-meshheading:11055333-Kinetics,
pubmed-meshheading:11055333-Naltrexone,
pubmed-meshheading:11055333-Narcotic Antagonists,
pubmed-meshheading:11055333-Pyrrolidines,
pubmed-meshheading:11055333-Receptors, Opioid, kappa,
pubmed-meshheading:11055333-Structure-Activity Relationship
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pubmed:year |
2000
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pubmed:articleTitle |
Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series.
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pubmed:affiliation |
School of Chemistry, University of Bristol, UK.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
|