rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
1-2
|
pubmed:dateCreated |
1992-3-31
|
pubmed:abstractText |
Naphthoquinones are known to inhibit 5-lipoxygenase. In particular, CGS 8515 (methyl 2-[(3,4-dihydro-3,4-dioxo-1-naphthalenyl)amino]benzoate) has been studied in detail. However this potent and selective 5-lipoxygenase inhibitor has a short duration of action and poor bioavailability. To improve the duration of action we have prepared a series of carbon substituted naphthoquinones. Several members of this series have demonstrated potent in vitro inhibition of 5-LO (IC50's less than 10(-6) M) and at doses of 1 mg/kg iv completely inhibited LTB4 production measured in ex vivo A23187-stimulated blood from dogs. The duration of action measured by the ex vivo assay was improved up to threefold over CGS 8515.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Sep
|
pubmed:issn |
0065-4299
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:volume |
34
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
145-7
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:1665288-Animals,
pubmed-meshheading:1665288-Anthranilic Acids,
pubmed-meshheading:1665288-Biological Availability,
pubmed-meshheading:1665288-Calcimycin,
pubmed-meshheading:1665288-Dogs,
pubmed-meshheading:1665288-Female,
pubmed-meshheading:1665288-Guinea Pigs,
pubmed-meshheading:1665288-Half-Life,
pubmed-meshheading:1665288-Leukotriene B4,
pubmed-meshheading:1665288-Lipoxygenase Inhibitors,
pubmed-meshheading:1665288-Male,
pubmed-meshheading:1665288-N-Formylmethionine Leucyl-Phenylalanine,
pubmed-meshheading:1665288-Naphthoquinones,
pubmed-meshheading:1665288-Radioimmunoassay
|
pubmed:year |
1991
|
pubmed:articleTitle |
Leukotriene biosynthesis inhibition by aryl and aroyl substituted naphthoquinones.
|
pubmed:affiliation |
Research Department, CIBA-GEIGY Corp., Summit, NJ 07901.
|
pubmed:publicationType |
Journal Article,
In Vitro
|