rdf:type |
|
lifeskim:mentions |
umls-concept:C0023688,
umls-concept:C0205549,
umls-concept:C0242402,
umls-concept:C0456378,
umls-concept:C1167622,
umls-concept:C1510411,
umls-concept:C1510827,
umls-concept:C1533691,
umls-concept:C1875307,
umls-concept:C1979963,
umls-concept:C2003903
|
pubmed:issue |
14
|
pubmed:dateCreated |
2003-6-26
|
pubmed:abstractText |
In investigation of the effects of 14-substitution in the indolomorphinan series of delta-selective opioid ligands, 5,14-bridged indolomorphinans (4) were prepared from the equivalent dihydrothebainone acid-catalyzed rearrangement products of the dihydrothevinols. Though the new ligands generally had low affinity for opioid receptors and no delta-selectivity, 4b had high kappa-affinity and substantial selectivity which was also seen in the precursor morphinanone (3b). This indicates that the methylbenzylidene-substituted bridge in these compounds is a dominant kappa-opioid receptor binding motif.
|
pubmed:grant |
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Bridged Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Indoles,
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/Morphinans,
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
|
pubmed:status |
MEDLINE
|
pubmed:month |
Jul
|
pubmed:issn |
0022-2623
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:day |
3
|
pubmed:volume |
46
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
3174-7
|
pubmed:dateRevised |
2007-11-14
|
pubmed:meshHeading |
pubmed-meshheading:12825957-Animals,
pubmed-meshheading:12825957-Bridged Compounds,
pubmed-meshheading:12825957-CHO Cells,
pubmed-meshheading:12825957-Cricetinae,
pubmed-meshheading:12825957-Indoles,
pubmed-meshheading:12825957-Ligands,
pubmed-meshheading:12825957-Morphinans,
pubmed-meshheading:12825957-Receptors, Opioid, delta,
pubmed-meshheading:12825957-Receptors, Opioid, kappa,
pubmed-meshheading:12825957-Receptors, Opioid, mu
|
pubmed:year |
2003
|
pubmed:articleTitle |
Opioid binding and in vitro profiles of a series of 4-hdroxy-3-methoxyindolomorphinans. Transformation of a delta-selective ligand into a high affinity kappa-selective ligand by introduction of a 5,14-substituted bridge.
|
pubmed:affiliation |
Department of Pharmacy and Pharmacology, University of Bath, Bath, BA2 7AY, UK.
|
pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
|