Endothelin Receptors and Receptor Antagonists

  • Andrew S. Tasker
  • David M. Pollock


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.


Atrial Natriuretic Peptide Rabbit Pulmonary Artery Thiazolyl Amino Amino Benzene Sulfonamide Rabbit Renal Artery 
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© Springer-Verlag Berlin Heidelberg 1998

Authors and Affiliations

  • Andrew S. Tasker
  • David M. Pollock

There are no affiliations available

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