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Endothelin Receptors and Receptor Antagonists

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Endothelin Receptors and Signaling Mechanisms

Abstract

Multiple receptor subtypes for endothelin have been identified in pharmacological studies both in vitro and in vivo. As can be evidenced in the study by Yanagisawa et al, at least two receptor subtypes may be responsible for the biphasic nature of the hemodynamic response to intravenous injection of ET-1: a transient hypotension followed by a sustained increase in arterial pressure.1 ET-1 and ET-2 are more active than ET-3 as pressor agents and as constrictors of many isolated vascular preparations.2 ET-1 and ET-3 have similar potencies in terms of transient hypotensive effects that are thought to be mediated by the release of nitric oxide and/or prostaglandins.3,4 These results led to the initial sub-classification of ET receptors as ETA (ET-1-selective located on vascular smooth muscle) and ETB (nonisopeptide-selective located on endothelial cells) which are generally responsible for vasoconstriction and vasodilation, respectively.

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Authors
  1. Andrew S. Tasker
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  2. David M. Pollock
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Editors and Affiliations

  1. Vascular Biology Center, Medical College of Georgia, Augusta, Georgia, USA

    David M. Pollock Ph.D.

  2. Department Molecular and Cellular Physiology, University of Cincinnati Medical Center Cincinnati, Ohio, USA

    Robert F. Highsmith Ph.D.

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Tasker, A.S., Pollock, D.M. (1998). Endothelin Receptors and Receptor Antagonists. In: Pollock, D.M., Highsmith, R.F. (eds) Endothelin Receptors and Signaling Mechanisms. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-662-11672-2_2

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  • DOI: https://doi.org/10.1007/978-3-662-11672-2_2

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