Linked Life Data

17004724

Source:http://linkedlifedata.com/resource/pubmed/id/17004724

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
20
pubmed:dateCreated
2006-9-28
pubmed:abstractText
The 14-aminodihydromorphinone and codeinone series of opioid ligands have produced a number of ligands of substantial interest. To investigate the importance of the 14-substituent, a series of analogues in which the side chain length is varied and the amide and alkene functions are reduced have been prepared. Binding affinity, particularly at the mu-opioid receptor (MOR), was largely determined by the aromatic group of the side chain. In the [35S]GTPgammaS functional assay, the ligands having a three-carbon side chain were more potent antagonists than their longer chain counterparts, while shorter, two-carbon chain analogues were of higher MOR efficacy, an effect that was confirmed in vivo. Wash-resistant binding was observed within this series and appeared to be unrelated to side-chain length.
pubmed:grant
pubmed:commentsCorrections
http://linkedlifedata.com/resource/pubmed/commentcorrection/17004724-10945843, http://linkedlifedata.com/resource/pubmed/commentcorrection/17004724-10966754, http://linkedlifedata.com/resource/pubmed/commentcorrection/17004724-11779034, http://linkedlifedata.com/resource/pubmed/commentcorrection/17004724-16367983, http://linkedlifedata.com/resource/pubmed/commentcorrection/17004724-2641054, http://linkedlifedata.com/resource/pubmed/commentcorrection/17004724-3151920, http://linkedlifedata.com/resource/pubmed/commentcorrection/17004724-6095280, http://linkedlifedata.com/resource/pubmed/commentcorrection/17004724-7693944, http://linkedlifedata.com/resource/pubmed/commentcorrection/17004724-7723747, http://linkedlifedata.com/resource/pubmed/commentcorrection/17004724-8742788, http://linkedlifedata.com/resource/pubmed/commentcorrection/17004724-8858971
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Oct
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:day
5
pubmed:volume
49
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
6104-10
pubmed:dateRevised
2011-9-26
pubmed:meshHeading
pubmed:year
2006
pubmed:articleTitle
Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
pubmed:affiliation
University of Bristol, Cantock's Close, Bristol, BS8 1TS, United Kingdom.
pubmed:publicationType
Journal Article, Research Support, N.I.H., Extramural