Vasopressin Receptor Agonists Small Molecules and Peptides

Vasopressin receptors are a group of G-protein-coupled receptors that mediate vasoconstriction, antidiuresis and ACTH release. They are currently divided into three subtypes, V_1A, V_1B and V₂ and are closely related to oxytocin receptors (OT).

V_1A is coupled to G_q/11 proteins and is found at high density on smooth muscle cells. It is involved in regulation of blood pressure through arterial vasoconstriction and has been found to stimulate VEGF secretion. V_1B is located in the hypothalamus, where it controls ACTH secretion, and in the pancreas, where it is involved in insulin release. V₂ is coupled to G_s proteins and is found exclusively on the basolateral membrane of collecting duct cells in the kidney, where it regulates water excretion.