Endothelin pp 189-222 | Cite as

The Development of Specific Endothelin-Receptor Antagonists

  • Timothy D. Warner
Part of the Contemporary Biomedicine book series (CB)


The endothelins (ETs) (1,2) are produced and active in almost all tissues. However, they are best known for their effects within the cardiovascular system, where they are potent vasoconstrictors and pressor agents, although there may also be accompanying vasodilatation, particularly at low concentrations (2,3). The ETs also have numerous other effects, such as stimulating the release of autacoids and hormones, contracting nonvascular smooth muscle, potentiating and reducing neurotransmitter release, decreasing glomerular filtration, acting as cardiac inotropes and chronotropes, and increasing cell growth and division (3–11). Despite this wide variety of effects, much endothelin research has examined the regulatory effects of the endothelins in the cardiovascular system, and the production of ET-receptor antagonists has principally been aimed at generating compounds that will reduce the deleterious effects of the endothelins in vascular pathologies ranging from hypertension to renal failure and stroke.


Nonselective Antagonist Nonvascular Smooth Muscle Postischemic Acute Renal Failure Asterric Acid 
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© Springer Science+Business Media New York 1998

Authors and Affiliations

  • Timothy D. Warner

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