トロンボキサンA2合成酵素阻害剤と受容体拮抗剤

概要

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As successive discoveries were made of thromboxane A2, prostacyclin, and the leukotrienes from 1975 to 1979, the physiological and pathological roles of the arachidonate cascade metabolites were clarified. With these discoveries as a turning point, novel concepts for designing new drugs which specifically control and manipulate the metabolites have rapidly grown and developed. Any new approach to treating and preventing cardio- and cerebro- vascular diseases requires urgent and careful evaluation. Recent research into thromboxane synthetase inhibitors (TXSI) and thromboxane receptor antagonists (TXRA) has focussed attention mainly on platelets and blood vessel walls, and the interaction between the two. Some TXSI and TXRA have been studied in a variety of in vitro systems and animal models, and are now in various stages of clinical evaluation. In the present review, TXSI, TXRA, and the structure-activity relationships are described together with the results of our experiments on this subjects.
社団法人有機合成化学協会の論文