rdf:type |
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lifeskim:mentions |
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pubmed:issue |
5
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pubmed:dateCreated |
2001-3-26
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pubmed:abstractText |
Unexpectedly high affinity for opioid receptors has been observed for a novel series of cyclazocine analogues where the prototypic 8-OH was replaced by a carboxamido group. For mu and kappa opioid receptors, the primary carboxamido derivative of cyclazocine ((+/-)-15) displayed high affinity (Ki=0.41 and 0.53 nM, respectively) nearly comparable to cyclazocine. A high enantiopreference ((2R,6R,11R)-) for binding was also observed. Compound (+/-)-15 also displayed potent antinociception activity in mice when administered icv.
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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/Amides,
http://linkedlifedata.com/resource/pubmed/chemical/Analgesics, Non-Narcotic,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclazocine,
http://linkedlifedata.com/resource/pubmed/chemical/Narcotic Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, kappa,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, mu
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0960-894X
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pubmed:author |
|
pubmed:issnType |
Print
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pubmed:day |
12
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pubmed:volume |
11
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
623-6
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:11266156-Amides,
pubmed-meshheading:11266156-Analgesics, Non-Narcotic,
pubmed-meshheading:11266156-Animals,
pubmed-meshheading:11266156-Cyclazocine,
pubmed-meshheading:11266156-Mice,
pubmed-meshheading:11266156-Molecular Structure,
pubmed-meshheading:11266156-Narcotic Antagonists,
pubmed-meshheading:11266156-Radioligand Assay,
pubmed-meshheading:11266156-Receptors, Opioid, kappa,
pubmed-meshheading:11266156-Receptors, Opioid, mu,
pubmed-meshheading:11266156-Structure-Activity Relationship
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pubmed:year |
2001
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pubmed:articleTitle |
8-Carboxamidocyclazocine analogues: redefining the structure-activity relationships of 2,6-methano-3-benzazocines.
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pubmed:affiliation |
Department of Chemistry, Rensselaer Polytechnic Institute, Troy, NY 12180, USA. wentmp@rpi.edu
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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