Linked Life Data

19362480

Source:http://linkedlifedata.com/resource/pubmed/id/19362480

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
10
pubmed:dateCreated
2009-5-4
pubmed:abstractText
We re-examined the accessory site of the 4,5-epoxymorphinan skeleton by camdas conformational analysis in an effort to deign novel delta opioid receptor antagonists. We synthesized three novel compounds (SN-11, 23 and 28) with a 10-methylene bridge and without a 4,5-epoxy ring. Among them, compounds SN-23 (17-isobutyl derivative) and SN-28 (17-methyl derivative) showed very strong agonist activity (over 10 times more than TAN-67). SN-28 also showed high delta selectivity. The delta agonist activity of SN-23 was weaker than that of SN-28, but in terms of the delta selectivity, SN-23 was higher than that of SN-28. These unexpected results indicated that the 4,5-epoxy ring, but not the 10-methylene bridge, was an accessory site in delta opioid receptor agonists.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
May
pubmed:issn
1464-3405
pubmed:author
pubmed:issnType
Electronic
pubmed:day
15
pubmed:volume
19
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
2792-5
pubmed:meshHeading
pubmed:year
2009
pubmed:articleTitle
Design and synthesis of novel delta opioid receptor agonists and their pharmacologies.
pubmed:affiliation
Department of Medicinal Chemistry, Kitasato University, Shirokane, Minato-ku, Tokyo, Japan. nagaseh@pharm.kitasato-u.ac.jp
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't