Human Arginine Vasopressin Receptor 2 Reporter Assay System

This is an all-inclusive cell-based luciferase reporter assay kit targeting the Human Arginine Vasopressin Receptor 2 (AVPR2). INDIGO’s AVPR1B reporter assay utilizes proprietary mammalian cells that have been engineered to provide constitutive expression of the AVPR2. In addition to AVPR2 Reporter Cells, this kit provides two optimized media for use during cell culture and in diluting the user’s test samples, a reference agonist, Luciferase Detection Reagent, and a cell culture-ready assay plate. The principal application of this assay is in the screening of test samples to quantify any functional activity, either agonist or antagonist, that they may exert against AVPR2. This kit provides researchers with clear, reproducible results, exceptional cell viability post-thaw, and consistent results lot to lot. Kits must be stored at -80C. Do not store in liquid nitrogen. Note: reporter cells cannot be refrozen or maintained in extended culture..

The Arginine Vasopressin Receptor 2 (AVPR2), also known as the V2 receptor, is a member of the family of G-Protein-coupled receptors (GPCR). There are three subtypes of vasopressin receptors identified in humans, which are AVPR1A, AVPR1B and AVPR2.

The natural ligand of AVPR2 is vasopressin, which is synthesized in the hypothalamus and secreted into the posterior pituitary. Like the closely similar neuropeptide, oxytocin, vasopressin is a nine amino acid neuropeptide that is classified as an antidiuretic hormone (ADH). Release of vasopressin is mediated by stimuli such as hemorrhage or dehydration. When vasopressin binds to AVPR2, signal transduction is mediated through Gas GTP binding proteins, which activates adenylate cyclase to increase intracellular cAMP. This cascade further activates protein kinase A (PKA).

The most abundant expression of AVPR2 is found in the kidney. The main function of AVPR2 is to regulate water homeostasis in the body. Binding of vasopressin to the V2 receptor in the kidney stimulates cellular relocation of aquaporin 2 (AQP2) to the apical plasma membrane. This facilitates water reabsorption from primary urine. The impaired regulation of vasopressin causes a serious condition known as Diabetes insipidus (DI).

Besides as an antidiuretic factor, vasopressin is also known to regulate blood coagulation. Desmopressin has been used as a haemostatic drug for patients with hemophilia A by stimulating production of coagulant factor VIII. Interestingly, drug repurposing of desmopressin revealed the promising treatment for patients with osteosarcoma. In fact, AVPR2 has been detected in several cancers such as kidney, breast, colon and lungs.[INDIGO Catalog Nos. IB37201, IB37202]

WARNING This product is not for human or veterinary use.