Introduction: thromboxane in biological systems and the possible impact of its inhibition.
- M Verstraete
- British journal of clinical pharmacology
Dazoxiben. an imidazole-derived selective inhibitor of thromboxane A2 (TxA2) synthetase, prevented TxB2 synthesis in vitro in platelet-rich plasma from 1 6 normal subjects. Inhibition of TxB2 synthesis was accompanied by increased generation of PGE2. PGF ,. and PGD2. as shown by radioimmunoassay. thin-layer radiochromatography, and high-resolution gas chromatography-mass spectrometry. Even at dazoxiben concentrations (40-80 M) above those inhibiting TxB2 synthesis, platelet aggregation induced by threshold concentrations of arachidonic acid was inhibited in only 4 of 1 6 subjects. referred to as responders. The remaining 12 individuals were defined as nonresponders. The aggregating effect of arachidonic acid and of the prostaglandin-endoperoxide analog U-4661 9