Title: A potent inhibitor of thromboxane A2 biosynthesis in aggregating human blood platelets
Abstract: 1′(Isopropyl-2-indolyl)-3-pyridyl-3-ketone (L 8027) inhibited biosynthesis of thromboxane A2 from arachidonic acid in human platelet rich plasma and inhibited platelet aggregation. The anti-enzymic and anti-aggregating potencies of L 8027 were closely linked to each other and both of them were inversely proportional to concentrations of arachidonic acid which platelets were exposed to. Very low concentrations of L 8027 (0.1 fM – 40 nM) were needed to inhibit generation of thromboxane A2 and aggregation of platelets by the threshold pro-aggregatory concentrations of arachidonic acid. A concentration of 4 uM of L 8027 was sufficient to inhibit platelet aggregation induced by any concentration of arachidonic acid. L 8027 inhibits the activity of the arachidonate cyclo-oxygenase in many biological systems including platelets. However, unlike indomethacin L 8027 is a more potent thromboxane A2 synthetase inhibitor than a prostaglandin synthetase inhibitor.
Publication Year: 1977
Publication Date: 1977-02-01
Language: en
Type: article
Indexed In: ['crossref', 'pubmed']
Access and Citation
Cited By Count: 21
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