About Human Arginine Vasopressin Receptor 2 (AVPR2/V2R) Stable Cell Line

Arginine Vasopressin Receptor 2 (AVPR2), also known as Vasopressin V2 Receptor (V2R), is a Class A G protein-coupled receptor (GPCR) that serves as the principal receptor for arginine vasopressin (AVP), also known as antidiuretic hormone (ADH). AVPR2 is predominantly expressed in the collecting ducts of the kidney, where it plays a central role in regulating water reabsorption and maintaining fluid and electrolyte homeostasis. Upon activation by vasopressin, AVPR2 primarily couples to Gs proteins, stimulating adenylate cyclase activity and increasing intracellular cAMP levels. This signaling cascade promotes the translocation of aquaporin-2 (AQP2) water channels to the apical membrane of collecting duct cells, facilitating water reabsorption and urine concentration.

AVPR2 is essential for maintaining plasma osmolality, blood volume, and blood pressure. Defects in AVPR2 signaling are associated with several clinically important disorders, including nephrogenic diabetes insipidus (NDI), syndrome of inappropriate antidiuretic hormone secretion (SIADH), hyponatremia, heart failure, and polycystic kidney disease. Gain-of-function or loss-of-function mutations in AVPR2 can profoundly affect water balance, making the receptor a critical target in renal physiology and endocrine research. Therapeutic agents targeting AVPR2, including vasopressin analogs and V2 receptor antagonists (vaptans), are widely used in clinical medicine.

eEnzyme's Human AVPR2 Stable Cell Line provides a reliable and reproducible cellular platform for investigating AVPR2-mediated signaling pathways and evaluating receptor-targeted therapeutics. The cell line enables quantitative assessment of vasopressin analogs, agonists, antagonists, inverse agonists, and novel receptor modulators through cAMP assays, reporter gene assays, and other GPCR functional screening platforms. Researchers can utilize this stable cell line for receptor characterization, potency determination, lead optimization, biosimilar evaluation, and high-throughput screening applications supporting renal, cardiovascular, and endocrine drug discovery programs.

Applications of the AVPR2 Stable Cell Line

• AVPR2 receptor pharmacology studies
• Vasopressin signaling investigations
• Agonist and antagonist screening
• Nephrogenic diabetes insipidus research
• Kidney physiology and water balance studies
• SIADH and hyponatremia research
• cAMP and GPCR functional assays
• High-throughput screening applications

Biological Significance of AVPR2

AVPR2 is the primary regulator of renal water conservation and plays a fundamental role in maintaining body fluid homeostasis. Activation of the receptor by vasopressin stimulates cAMP-dependent signaling pathways that promote aquaporin-2 trafficking and water reabsorption in the kidney collecting ducts, allowing the body to concentrate urine and conserve water during dehydration. Mutations in AVPR2 are a major cause of congenital nephrogenic diabetes insipidus, while excessive AVPR2 signaling contributes to water retention disorders such as SIADH. The receptor is also an important therapeutic target in heart failure, cirrhosis, autosomal dominant polycystic kidney disease (ADPKD), and electrolyte imbalance disorders. Because of its critical role in renal physiology, endocrine regulation, and fluid balance, AVPR2 remains a highly important target for nephrology research and GPCR-focused drug discovery. The AVPR2 Stable Cell Line provides a valuable tool for studying vasopressin receptor biology and advancing the development of next-generation therapeutics targeting renal and fluid homeostasis disorders.