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New developments on thromboxane and prostacyclin modulators - Part I: Thromboxane modulators

Dogne, JM, de Leval, X, Hanson, J, Frederich, M, Lambermont, B, Ghuysen, A, Casini, Angela, Masereel, B, Ruan, KH, Pirotte, B and Kolh, P 2004. New developments on thromboxane and prostacyclin modulators - Part I: Thromboxane modulators. Current Medicinal Chemistry 11 (10) , pp. 1223-1241.

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The pathogenesis of numerous cardiovascular, pulmonary, inflammatory, and thromboembolic diseases can be related to arachidonic acid (AA) metabolites. One of these bioactive metabolites of particular importance is thromboxane A2 (TXA2). It is produced by the action of thromboxane synthase on the prostaglandin endoperoxide H2 (PGH2), which results from the enzymatic degradation of AA by the cyclooxygenases. TXA2 is a potent inducer of platelet aggregation, vasoconstriction and bronchoconstriction. It is involved in a series of major pathophysiological states such as asthma, myocardial ischemia, pulmonary hypertension, and thromboembolic disorders. Therefore, TXA2 receptor antagonists, thromboxane synthase inhibitors and drugs combining both properties have been developed by several pharmaceutical companies since the early 1980s. Several compounds have been launched on the market and others are under clinical evaluation. Moreover, the recent literature reported the interest of thromboxane modulators, which combine another pharmacological activity such as, platelet activating factor antagonism, angiotensin II antagonism, or 5-lipoxygenase inhibition. In this review, we will propose a description of the recently described thromboxane modulators of major interest from both a pharmacological and a chemical point of view.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Chemistry
Subjects: Q Science > QD Chemistry
R Medicine > RM Therapeutics. Pharmacology
Uncontrolled Keywords: Arachidonic acid; Prostanoids; Thromboxane A2; Thromboxane receptor antagonist; Thromboxane synthase; Thromboxane synthase inhibitor
Publisher: Bentham Science Publishers Ltd
ISSN: 0929-8673
Last Modified: 04 Jun 2017 08:49

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