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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
23
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pubmed:dateCreated |
1983-3-11
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pubmed:abstractText |
In vitro, 5-fluoropentane-1,4-diamine and 5,5-difluoropentane-1,4-diamine are potent enzyme-activated inhibitors of rat liver ornithine decarboxylase (EC 4.1.1.17). The two alpha-fluoromethyl derivatives of putrescine activate to different degrees S-adenosyl-L-methionine decarboxylase (EC 4.1.1.50). The difluoromethyl derivative differs from the monofluoromethyl derivative in that it is not a substrate of diamine oxidase (EC 1.4.3.6), but is a better substrate of mitochondrial monoamine oxidase (EC 1.4.3.4) than the monofluoromethyl derivative. In vivo, a single i.p. injection of 200 mg/kg of 5-fluoropentane-1,4-diamine to rats causes a marked decrease of the ornithine decarboxylase activity in the ventral prostate and to a lesser extent in the thymus, whereas 5,5-difluoropentane-1,4-diamine causes only a slight decrease of this enzyme activity in the prostate and does not affect it in the thymus. Both compounds produce a decrease of 4-aminobutyrate: 2-oxoglutarate aminotransferase (EC 2.6.1.19) activity in the brain. The differences observed between the biochemical properties of the two alpha-fluoromethyl derivatives of putrescine are discussed in relation to the pKa value of the alpha-amino group which decreases from 7.75 for 5-fluoropentane-1,4-diamine to 6.4 for 5,5-difluoropentane-1,4-diamine.
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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 |
Dec
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pubmed:issn |
0006-2952
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
1
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pubmed:volume |
31
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pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
3871-8
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:7159464-Animals,
pubmed-meshheading:7159464-Carboxy-Lyases,
pubmed-meshheading:7159464-Chemical Phenomena,
pubmed-meshheading:7159464-Chemistry,
pubmed-meshheading:7159464-Kinetics,
pubmed-meshheading:7159464-Liver,
pubmed-meshheading:7159464-Male,
pubmed-meshheading:7159464-Ornithine Decarboxylase,
pubmed-meshheading:7159464-Prostate,
pubmed-meshheading:7159464-Putrescine,
pubmed-meshheading:7159464-Rats,
pubmed-meshheading:7159464-Rats, Inbred Strains,
pubmed-meshheading:7159464-Testis,
pubmed-meshheading:7159464-Thymus Gland,
pubmed-meshheading:7159464-Time Factors
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pubmed:year |
1982
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pubmed:articleTitle |
alpha-Monofluoromethyl and alpha-difluoromethyl putrescine as ornithine decarboxylase inhibitors: in vitro and in vivo biochemical properties.
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pubmed:publicationType |
Journal Article
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