AQP2 Inhibitors

Common AQP2 Inhibitors include, but are not limited to Lithium CAS 7439-93-2, Amiloride • HCl CAS 2016-88-8, Tolvaptan CAS 150683-30-0, Furosemide CAS 54-31-9 and Hydrochlorothiazide CAS 58-93-5.

Aquaporin-2 (AQP2) is one of the members of the aquaporin family, a group of small integral membrane proteins that function as water channels. These proteins play pivotal roles in regulating water transport across cell membranes in various tissues. AQP2, in particular, is primarily expressed in the principal cells of the kidney's collecting ducts. The localization and abundance of AQP2 at the apical plasma membrane determine the water reabsorption rate from the urine, which is critical for maintaining body water homeostasis. AQP2 trafficking to the apical membrane, and thus its activity, is primarily regulated by the antidiuretic hormone vasopressin. Vasopressin binds to its receptor (V2R) on the basolateral membrane of the principal cells, leading to a signaling cascade that results in AQP2's insertion into the apical membrane, thereby increasing water permeability and reabsorption.

AQP2 inhibitors are molecules specifically designed to reduce the activity or expression of AQP2, thereby influencing the water permeability of the collecting ducts. These inhibitors can act through various mechanisms. Some might directly block the water channel activity of AQP2, while others might interfere with the signaling pathways that control AQP2 trafficking to the cell surface. Yet, another group might hinder the transcription or translation of the AQP2 gene. By inhibiting AQP2's function, these molecules play a role in modulating the balance of water reabsorption in the kidneys, which can influence urine concentration and volume. The study of AQP2 inhibitors not only deepens our understanding of renal water regulation and the molecular biology of aquaporins but also sheds light on the intricate mechanisms governing cellular water transport and balance across various tissues.