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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
19
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pubmed:dateCreated |
1985-11-13
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pubmed:abstractText |
Histidine decarboxylase (HDC) activity in Ficoll-Hypaque purified human peripheral blood leukocytes (PBL) was determined by measuring the formation of [3H]histamine from L-[3H]histidine. HDC activity was inhibited in vitro to more than 90% by (S)-alpha-fluoromethylhistidine (alpha-FMH) at concentrations of 10(-5) M and above. Both polymorphonuclear and mononuclear cells possessed HDC activity, but on a per cell basis the former had several-fold higher enzyme activity than the latter. In safety and tolerability studies, alpha-FMH was administered orally to healthy human subjects twice daily for 7 days at doses of 2.5, 10, 50 and 100 mg per person. A dose-dependent inhibition of HDC activity was observed in PBL that were isolated both at 12 hr after administration of the first dose of alpha-FMH and after treatment for 1 week. At the 50 and 100 mg doses of alpha-FMH, there was complete inhibition of HDC activity and partial inhibition at the 10 mg dose. Twenty-four hours after the last dose, HDC activity had recovered to 64-100%, 44-46%, and 30-52% of control values in subjects that received 10, 50 and 100 mg alpha-FMH respectively.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Carboxy-Lyases,
http://linkedlifedata.com/resource/pubmed/chemical/Histamine,
http://linkedlifedata.com/resource/pubmed/chemical/Histidine,
http://linkedlifedata.com/resource/pubmed/chemical/Histidine Decarboxylase,
http://linkedlifedata.com/resource/pubmed/chemical/Methylhistidines,
http://linkedlifedata.com/resource/pubmed/chemical/alpha-fluoromethylhistidine
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pubmed:status |
MEDLINE
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pubmed:month |
Oct
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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 |
34
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3509-15
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:4052095-Carboxy-Lyases,
pubmed-meshheading:4052095-Histamine,
pubmed-meshheading:4052095-Histidine,
pubmed-meshheading:4052095-Histidine Decarboxylase,
pubmed-meshheading:4052095-Humans,
pubmed-meshheading:4052095-Leukocytes,
pubmed-meshheading:4052095-Lymphocytes,
pubmed-meshheading:4052095-Male,
pubmed-meshheading:4052095-Methylhistidines,
pubmed-meshheading:4052095-Monocytes,
pubmed-meshheading:4052095-Neutrophils
|
pubmed:year |
1985
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pubmed:articleTitle |
In vivo and in vitro inhibition of human histidine decarboxylase by (S)-alpha-fluoromethylhistidine.
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pubmed:publicationType |
Journal Article,
Comparative Study
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