Vasopressin receptor antagonism--a therapeutic option in heart failure and hypertension

Exp Physiol. 2000 Mar:85 Spec No:259S-265S. doi: 10.1111/j.1469-445x.2000.tb00031.x.


The precise role of vasopressin in the pathophysiology of cardiovascular disease is controversial, but this peptide hormone is important for several reasons. Firstly, circulating concentrations of vasopressin are elevated in heart failure and some forms of hypertension. Secondly, there is evidence that vasopressin is synthesized not only in the hypophysial-pituitary axis but also in peripheral tissues including the heart where it acts as a paracrine hormone. Thirdly, vasopressin has vasoconstrictor, mitogenic, hyperplastic and renal fluid retaining properties which, by analogy with angiotensin II, may have deleterious effects when present in chronic excess. Finally, the availability of orally active non-peptide vasopressin receptor antagonists allows vasopressin receptor antagonism to be considered as a therapeutic option in cardiovascular disease.

Publication types

  • Review

MeSH terms

  • Antidiuretic Hormone Receptor Antagonists*
  • Benzazepines / therapeutic use*
  • Heart Failure / drug therapy*
  • Heart Failure / physiopathology
  • Humans
  • Hypertension / drug therapy*
  • Hypertension / physiopathology
  • Morpholines / therapeutic use
  • Receptors, Vasopressin / physiology*
  • Spiro Compounds / therapeutic use
  • Tolvaptan


  • Antidiuretic Hormone Receptor Antagonists
  • Benzazepines
  • Morpholines
  • Receptors, Vasopressin
  • Spiro Compounds
  • mozavaptan
  • Tolvaptan
  • satavaptan