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: thromboxane, prostacyclin modulators, prostacyclin, hypertension, stroke, atherosclerosis, myocardial infarction
Current Medicinal Chemistry
Title: New Developments on Thromboxane and Prostacyclin Modulators Part II: Prostacyclin Modulators
Volume: 11 Issue: 10
Author(s): Xavier de Leval, Julien Hanson, Jean-Louis David, Bernard Masereel, Bernard Pirotte and Jean-Michel Dogne
Affiliation:
Keywords: thromboxane, prostacyclin modulators, prostacyclin, hypertension, stroke, atherosclerosis, myocardial infarction
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.
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Leval de Xavier, Hanson Julien, David Jean-Louis, Masereel Bernard, Pirotte Bernard and Dogne Jean-Michel, New Developments on Thromboxane and Prostacyclin Modulators Part II: Prostacyclin Modulators, Current Medicinal Chemistry 2004; 11 (10) . https://dx.doi.org/10.2174/0929867043365279
DOI https://dx.doi.org/10.2174/0929867043365279 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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