Investigational vasopressin receptor modulators in the pipeline

Abstract

The vasopressin system is complex and interacts with the central nervous, cardiovascular, renal, and hematological systems. Vasopressin plays an important role in the control of blood osmolarity and vascular tone, but is also involved in many other physiological events, which are mediated mainly via three types of vasopressin receptor: V₁R, V₂R, and V₃R. V₁R primarily mediate the vascular, and V₂R the aquaretic, effects of vasopressin. Vasopressin may also interact with other receptors, like adrenergic and angiotensin-II receptors, or with distinct biological pathways, including those of nitric oxide and the K_ATP channel. There are numerous clinical situations where vasopressin receptor modulators (agonists or antagonists) could be used. Currently, vasopressin and terlipressin are most commonly used to stimulate V₁R in vasodilatory shock and cardiac arrest, while desmopressin, a synthetic analogue of vasopressin, acts on V₂R; but new molecules are becoming available in the treatment of inappropriate antidiuretic hormone (ADH) secretion.

Keywords::

• terlipressin
• tolvaptan
• vasopressin
• vasopressin receptor agonist
• vasopressin receptor antagonist

Notes