V2 Receptor  Inhibitor

AGN-190851 is a potent and selective agonist of α₂-adrenergic receptor (α₂ adrenoceptor). AGN-190851 induces dose-dependent water diuresis in rats, and inhibits vasopressin V2 receptor in a species-dependent manner in vitro, thereby suppressing cAMP production. AGN-190851 enhances the contraction of porcine myometrium. AGN 190851 can be used in studies on renal diuretic mechanisms, pharmacology of α₂-adrenergic receptor subtypes, and parturition.

Pecavaptan, a chemical probe, is an orally active and dual antagonist of V1a/V2 receptor (K_i=0.5 nM and 0.6 nM for human, respectively). Pecavaptan promotes an increase in urine production, which reduces the associated symptoms of water retention and edema.

DM-4111, one of the major monohydroxyl metabolites of Tolvaptan (HY-17000), is a potent vasopressin V₂ receptor inhibitor. DM-4111 inhibits water reabsorption in the renal tubules, thereby promoting the excretion of electrolyte-free water. DM-4111 is promising for research of cardiovascular diseases.