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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
11
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pubmed:dateCreated |
2003-5-16
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pubmed:abstractText |
High affinity binding for mu and kappa opioid receptors has been observed in analogues of cyclazocine, ethylketocyclazocine and naltrexone where the prototypic (of opiates) phenolic OH group was replaced with a formamide (-NHCHO) group. For the 8-formamide analogue of cyclazocine, binding is highly enantiospecific (eudismic ratios approximately 2000 for mu and kappa) with K(i) values </=1 nM observed for the (2R,6R,11R)-isomer, (-)-4. A preliminary SAR revealed that affinity is very sensitive to substitution on the formamide appendage.
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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 |
Jun
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pubmed:issn |
0960-894X
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
2
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pubmed:volume |
13
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1911-4
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:12749896-Analgesics, Non-Narcotic,
pubmed-meshheading:12749896-Animals,
pubmed-meshheading:12749896-Brain,
pubmed-meshheading:12749896-Cyclazocine,
pubmed-meshheading:12749896-Formamides,
pubmed-meshheading:12749896-Guinea Pigs,
pubmed-meshheading:12749896-Kinetics,
pubmed-meshheading:12749896-Radioligand Assay,
pubmed-meshheading:12749896-Receptors, Opioid, kappa,
pubmed-meshheading:12749896-Receptors, Opioid, mu,
pubmed-meshheading:12749896-Stereoisomerism,
pubmed-meshheading:12749896-Structure-Activity Relationship
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pubmed:year |
2003
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pubmed:articleTitle |
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 2: 8-formamidocyclazocine analogues.
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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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