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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
2
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pubmed:dateCreated |
1980-5-23
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pubmed:abstractText |
A series of 8-alkyl-3-methoxy-17-methylmorphinan-6-ones (3C) and -isomorphinan-6-ones (3T) were prepared by conjugate addition of lithium dialkylcuprates to the corresponding 7,8-didehydro-6-ones 2C and 2T. These 17-methyl compounds were potent analgesics and were converted to mixed narcotic agonists-antagonists 7-10, by replacement of the 17-methyl groups with cycloalkylmethyl moieties. The 8 substituent modified the type of activity observed. One of these compounds, 17-(cyclobutylmethyl)-3-hydroxy-8 beta-methylmorphinan-6-one (10Ca), had an agonist-antagonist ratio of 0.1. Compound 10Ca did not support or cause dependence in rats. This compound, however, appeared to be a typical narcotic agent in morphine-dependent monkeys.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
23
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
174-9
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:6767032-Acetic Acids,
pubmed-meshheading:6767032-Analgesics,
pubmed-meshheading:6767032-Animals,
pubmed-meshheading:6767032-Haplorhini,
pubmed-meshheading:6767032-Humans,
pubmed-meshheading:6767032-Mice,
pubmed-meshheading:6767032-Morphinans,
pubmed-meshheading:6767032-Morphine Dependence,
pubmed-meshheading:6767032-Narcotic Antagonists,
pubmed-meshheading:6767032-Rats,
pubmed-meshheading:6767032-Reaction Time,
pubmed-meshheading:6767032-Structure-Activity Relationship,
pubmed-meshheading:6767032-Substance Withdrawal Syndrome,
pubmed-meshheading:6767032-Substance-Related Disorders
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pubmed:year |
1980
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pubmed:articleTitle |
Analgesic narcotic antagonists. 2. 8-Alkymorphinan-6-ones.
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pubmed:publicationType |
Journal Article
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