Chapter

Endothelin and Its Inhibitors

Volume 152 of the series Handbook of Experimental Pharmacology pp 155-208

Endothelin-Converting Enzyme Inhibitors and their Effects

  • B. Battistini
  • , A. Y. Jeng

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Abstract

Previous chapters in this handbook have reviewed extensively the biochemistry and pharmacology of the family of three endothelin (ET) isopeptides and their respective precursors. Pathways responsible for the synthesis of ETs have also been introduced. In this chapter, these subjects as well as the existence and cellular/tissue localization of endothelin-converting enzyme (ECE) isoforms are nevertheless reviewed briefly as they are important in understanding the development of inhibitors of the synthesis of ET isopeptides. The major focus of the present chapter remains on the design and pharmacological properties of various types of ECE inhibitors and the effectiveness of these compounds in isolated cells, organs, tissues, and in animal models of human pathophysiology. An overall view of the comparative advantages and disadvantages of the use of ET receptor antagonists vs ECE inhibitors for the inhibition of the ET-mediated effects is also presented.