- Vasopressin Receptor Inhibitors (3)
|Catalog No.||Information||Product Use Citations||Product Validations|
Conivaptan HCl is an orally active, non-peptide, vasopressin V1A and V2 receptor antagonist, used in the treatment of euvolemic and hypervolemic hyponatremia.
Tolvaptan is an orally effective nonpeptide arginine vasopressin V2 receptor antagonist with IC50 of 3 nM, used to treat hyponatremia.
Immunoblots of inner medullas from control and tolvaptan-treated rats. Each lane was loaded with a sample from a different rat. Tolvaptan (2.5 mg/day) or vehicle was infused for 4 days. Loading: aquaporin-2 (AQP2), 15 μg; AQP3, 20 μg; AQP4, 25 μg; and urea transporter UT-A1, 25 μg. Values are normalized band densities covering all bands (means ± SE). *Statistical significance (P < 0.05, t-test).
Mozavaptan is a novel competitive vasopressin receptor antagonist for both V1 and V2 receptors with IC50 of 1.2 μM and 14 nM, respectively.