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New Trends in Thromboxane and Prostacyclin Modulators

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Abstract:

Thromboxane A 2 (TXA 2 ) and prostacyclin (PGI 2 ) are two labile products formed from arachidonic acid by the way of cyclooxygenase. An overproduction of thromboxane A 2 has been detected in a series of diseases whereby this prostanoid is assumed to contribute to the underlying pathomechanisms by its potent stimulation of platelet aggregation and smooth muscle contraction. This increased TXA 2 biosynthesis is frequently accompanied by a stimulation of prostacyclin formation which is one of the most potent inhibitors of platelet aggregation and smooth muscle contraction. Therefore, TXA 2 prostaglandin endoperoxide H 2 receptor antagonists, thromboxane synthase inhibitors and drugs which combine both activities have been developed with the aim to suppress the formation and/or the action of thromboxane A 2 . Since prostacyclin has been demonstrated to counterbalance the pathological effects of TXA 2 , several PGI 2 agonists have also been developed. This review will highlight the evolution and some of the latest findings in the field of prostacyclin and thromboxane A 2 modulators mainly those which are under clinical evaluation or marketed.

Keywords: Combined thromboxane A2 receptor antagonists; Non Prostanoid thromboxane A2 receptor antagonists; Prostanoid thromboxane A2 receptor antagonists; TXA2 PGH2 receptor antagonists TXRAs; TXA2 biosynthesis; TXSIs; prostacylin modulators; prostaglandin D2; prostaglandin E2; prostaglandin F2; prostaglandin G2; prostaglandin H2; prostaglandin endoperoxide H2 receptor antagonists; sulotroban; thormboxane synthase inhibitors; thromboxane A2 TXA2

Document Type: Review Article

DOI: http://dx.doi.org/10.2174/0929867003374868

Publication date: June 1, 2000

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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