rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
2
|
pubmed:dateCreated |
2002-1-10
|
pubmed:abstractText |
A new method for the preparation of N-benzylpyrrolomorphinans has been developed. Thus Michael reaction of the benzylimines of oxycodones and oxymorphones with nitrostyrenes gave a series of 4'-aryl-N-benzylpyrrolomorphinans. These were selective delta antagonists of much higher in vitro potency (with 5a having K(e) delta = <1 nM) than their binding affinities predicted. In mice in vivo assays 5a showed good delta antagonist activity in the anti-writhing analgesic assay and also inhibited delta agonist-induced convulsant activity.
|
pubmed:grant |
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Jan
|
pubmed:issn |
0022-2623
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:day |
17
|
pubmed:volume |
45
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
537-40
|
pubmed:dateRevised |
2007-11-14
|
pubmed:meshHeading |
pubmed-meshheading:11784158-Animals,
pubmed-meshheading:11784158-CHO Cells,
pubmed-meshheading:11784158-Cricetinae,
pubmed-meshheading:11784158-Humans,
pubmed-meshheading:11784158-Ligands,
pubmed-meshheading:11784158-Male,
pubmed-meshheading:11784158-Mice,
pubmed-meshheading:11784158-Morphinans,
pubmed-meshheading:11784158-Narcotic Antagonists,
pubmed-meshheading:11784158-Radioligand Assay,
pubmed-meshheading:11784158-Receptors, Opioid, delta,
pubmed-meshheading:11784158-Seizures,
pubmed-meshheading:11784158-Structure-Activity Relationship,
pubmed-meshheading:11784158-Transfection,
pubmed-meshheading:11784158-Vas Deferens
|
pubmed:year |
2002
|
pubmed:articleTitle |
4'-Arylpyrrolomorphinans: effect of a pyrrolo-N-benzyl substituent in enhancing delta-opioid antagonist activity.
|
pubmed:affiliation |
School of Chemistry, University of Bristol, Bristol BS8 1TS, UK.
|
pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, U.S. Gov't, P.H.S.
|