New Developments on Thromboxane and Prostacyclin Modulators Part II: Prostacyclin Modulators

Authors: Leval, Xavier d.; Hanson, Julien; David, Jean-Louis; Masereel, Bernard; Pirotte, Bernard; Dogne, Jean-Michel

Source: Current Medicinal Chemistry, Volume 11, Number 10, May 2004 , pp. 1243-1252(10)

Publisher: Bentham Science Publishers

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Abstract:

Prostacyclin (PGI2) is a potent endogenous inhibitor of platelet function and possesses a strong vasodilator effect. Furthermore, prostacyclin is currently presented as the physiologic antagonist of thromboxane A2 (TXA2), which exhibits pro-aggregatory and vasoconstrictor properties. So, the balance between PGI2 and TXA2 production is crucial for the cardiovascular system. Indeed, an imbalance in the production or effect of these products is deleterious for the circulatory system and can lead to characterized vascular diseases such as hypertension, stroke, atherosclerosis or myocardial infarction. Although the biological effects of PGI2 are considered to be clinically useful, its use as therapeutic agent is largely limited by both its chemical and metabolic instability. Actually, several prostacyclin agonists have been synthesized and pharmacologically evaluated. Among these, some have been clinically evaluated as therapeutic agents in several vascular diseases. This review focuses on the latest chemical and pharmacological developments in the field of the prostacyclin agonists.

Keywords: atherosclerosis; hypertension; myocardial infarction; prostacyclin; prostacyclin modulators; stroke; thromboxane

Document Type: Review Article

DOI: http://dx.doi.org/10.2174/0929867043365279

Affiliations: University of Liege, Department of Medicinal Chemistry, 1, avenue de l'Hopital, tour 4 (+5), B-4000 Liege (Belgium).

Publication date: May 1, 2004

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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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