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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
1990-6-7
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pubmed:abstractText |
Among nonsteroidal antiandrogens, mostly compounds of the Flutamide-type are described. For the development of new compounds with affinity to androgen receptors and antiandrogenic activity five new hydroxy-substituted phenyltetralines were prepared and tested. Synthesis was achieved by reaction of the respective 1-tetralones with phenyl magnesium bromides, dehydration of the carbinols, hydrogenation and ether cleavage. In addition to the expected affinity to estrogen receptors, especially the 6-OH, 4'-OH-substituted compound 11 showed an affinity to androgen receptors, too. Whereas none of the tested compounds had a marked estrogenicity, 11 and 15 (6-OH, 3'-OH) exerted antiestrogenic effects. Androgenic properties were not given. In the adult, intact mouse, 11 and 15 exhibited a pronounced inhibition of seminal vesicle weights concomitant with a reduction of the testosterone level. Since in castrated, androgen-substituted animals only relatively weak direct antiandrogenic effects were demonstrable, the antiandrogenic activity of these new phenyltetralines is more due to an inhibition of testosterone biosynthesis than to a direct, receptor-mediated effect.
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pubmed:language |
ger
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0365-6233
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
323
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
17-21
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:2334266-Animals,
pubmed-meshheading:2334266-Binding, Competitive,
pubmed-meshheading:2334266-Chemical Phenomena,
pubmed-meshheading:2334266-Chemistry,
pubmed-meshheading:2334266-Mice,
pubmed-meshheading:2334266-Naphthalenes,
pubmed-meshheading:2334266-Rats,
pubmed-meshheading:2334266-Receptors, Androgen,
pubmed-meshheading:2334266-Receptors, Estrogen,
pubmed-meshheading:2334266-Tetrahydronaphthalenes
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pubmed:year |
1990
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pubmed:articleTitle |
[Hydroxy substituted phenyltetralines: compounds with affinity for estrogen and androgen receptors].
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pubmed:affiliation |
Sonderforschungsbereich 234, Institut für Pharmazie, Lehrstuhl Pharmazeutische Chemie II, Universität Regensburg.
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pubmed:publicationType |
Journal Article,
English Abstract
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