Linked Life Data

7020379

Source:http://linkedlifedata.com/resource/pubmed/id/7020379

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
3
pubmed:dateCreated
1981-9-15
pubmed:abstractText
Several 3-(1-imidazolylmethyl) indoles were tested for inhibition of the microsomal enzymes which catalyse the biosynthesis of thromboxane A2, prostaglandin I2, and prostaglandin endoperoxides. These products were measured by bioassay to assess levels of enzyme activity. The highest activity against human blood platelet thromboxane A2-synthetase was obtained with 2-cyclopropyl-3(1-imidazolylmethyl) indole (IC50 1 x 10(-10) M). This compound also exhibited the highest activity against pig aorta prostaglandin I2-synthetase (IC50 8.4 x 10(-7) M). Of much more potential therapeutic interest, 2-isopropyl-3-(1-imidazolylmethyl) indole showed almost complete selectivity against thromboxane A2-synthetase. Both compounds exhibited IC50's of 2 x 10(-8) M against the latter enzyme but showed only weak effects (IC50's greater than 10(-4) M) against prostaglandin I2-synthetase and ram seminal vesicle PGH2-synthetase.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
May
pubmed:issn
0065-4299
pubmed:author
pubmed:issnType
Print
pubmed:volume
11
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
274-80
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1981
pubmed:articleTitle
3-(1-imidazolylmethyl) indoles: potent and selective inhibitors of human blood platelet thromboxane synthetase.
pubmed:publicationType
Journal Article, Comparative Study, In Vitro