Linked Life Data

6156240

Source:http://linkedlifedata.com/resource/pubmed/id/6156240

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
6
pubmed:dateCreated
1980-9-26
pubmed:abstractText
Two new long-acting hydrazone derivatives of 14-hydroxydihydromorphinones have been synthesized, oxymorphazone and naltrexazone. Both derivatives show high affinity for opiate binding sites in vitro, similar to naloxazone, the hydrazone analogue of naloxone. Sodium and manganese shifts imply that naltrexazone, like naloxazone, is a pure antagonist. By contrast, oxymorphazone inhibition of receptor binding is dramatically reduced by sodium and potentiated by manganese, suggesting it is an agonist. When given in vivo, all agents produce a significant inhibition of receptor binding for over 24 h despite extensive washing of the brain homogenates. Oxymorphone, naltrexone, and naloxone are without effect. Twenty-four hours after in vivo administration of oxymorphazone, 82% of mice are still analgetic compared to only 17% of oxymorphone-treated mice (p less than 0.005). Twenty-four hours after naltexazone or naloxazone treatment all mice were protected from morphine analgesia (12 mg/kg; p less than 0.005), while naltrexone- and naloxone-treated animals did not differ significantly from saline-treated controls.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jun
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:volume
23
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
674-6
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1980
pubmed:articleTitle
Long-acting opiate agonists and antagonists: 14-hydroxydihydromorphinone hydrazones.
pubmed:publicationType
Journal Article, In Vitro, Research Support, U.S. Gov't, P.H.S.