title: New developments on thromboxane and prostacyclin modulators part II: prostacyclin modulators.
abstract: Prostacyclin (PGI(2)) 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 A(2)(TXA(2)), which exhibits pro-aggregatory and vasoconstrictor properties. So, the balance between PGI(2) and TXA(2) 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 PGI(2) 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.
authors.affiliation: Natural and Synthetic Drugs Research Center, Department of Medicinal Chemistry, University of Liège, B-4000, Liège, Belgium. xdeleval@ulg.ac.be
authors.forename: Xavier
authors.initials: X
authors.lastname: de Leval
authors.forename: Julien
authors.initials: J
authors.lastname: Hanson
authors.forename: Jean-Louis
authors.initials: JL
authors.lastname: David
authors.forename: Bernard
authors.initials: B
authors.lastname: Masereel
authors.forename: Bernard
authors.initials: B
authors.lastname: Pirotte
authors.forename: Jean-Michel
authors.initials: JM
authors.lastname: Dogné
mesh_terms: D002319:Cardiovascular System / Q000187:drug effects* / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D011464:Epoprostenol / Q000819:agonists / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D013928:Thromboxane A2 / Q000037:antagonists & inhibitors / Q000502:physiology; D013931:Thromboxanes / Q000037:antagonists & inhibitors* / Q000502:physiology
chemical_list: D004791:Enzyme Inhibitors; D013931:Thromboxanes; D013928:Thromboxane A2; D011464:Epoprostenol