AAV ACTOne Gs-GPCR Assay Kit-AVPR2

The AAV ACTOne Gs-GPCR Assay Kit-AVPR2 is designed specifically for screening drugs/compounds that target the Arginine vasopressin receptor 2 (AVPR2) by combination AAV and ACTOne technologies.
Arginine vasopressin receptor 2 (officially called AVPR2), or vasopressin receptor 2 (V2R), is a G protein-coupled receptor (GPCR) primarily expressed in the kidneys, specifically in the renal collecting ducts. It is activated by the hormone vasopressin (antidiuretic hormone, ADH) and primarily couples with the Gs class of G proteins, leading to an increase in cyclic AMP (cAMP) levels. This signaling pathway promotes the insertion of aquaporin-2 water channels into the cell membrane, facilitating water reabsorption and concentrating urine. AVPR2 plays a crucial role in water homeostasis and blood pressure regulation. Mutations in the V2 receptor are associated with nephrogenic diabetes insipidus, a condition characterized by the kidney's inability to concentrate urine, leading to excessive urination and thirst. AVPR2 is also targeted by vasopressin receptor antagonists, which are used in the treatment of conditions like hyponatremia (low blood sodium levels).
This kit uses AAV vectors with a CMV promoter to co-express the AVPR2 and cyclic nucleotide-gated (CNG) channel, allowing researchers to conduct high-throughput screening and functional analysis of potential AVPR2-targeting compounds. The kit provides a sensitive and reliable method for evaluating the pharmacological properties of AVPR2 drugs, such as agonists and antagonists, in a live-cell environment.

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Background

ACTOne™ is the only high-throughput GPCR screening technology that can directly measure the intracellular changes of the secondary messenger cyclic AMP (cAMP) in living cells, in real-time. It uses a proprietary modified cyclic nucleotide-gated (CNG) channel, which is co-localized with adenylate cyclase at the plasma membrane, as a biosensor of cAMP activity. The CNG channel opens when the cAMP level near the plasma membrane increases, resulting in ion flux and cell membrane depolarization. The influx of cations through the CNG channel can be quantified using fluorescent ion indicators or membrane potential (MP) dyes. It provides information on real time intracellular cAMP changes and is highly sensitive. By combining kinetic and endpoint readouts, we are able to capture and analyze transient responses from endogenous GPCRs and weak responses caused by weak Gs or Gi coupled GPCR activities. Using ACTOne, we are able to detect the subcellular cAMP concentration changes directly caused by GPCR activation. Real-time kinetic readouts minimize artifacts, and provide greater content and more statistically relevant data. The intensity of signal increase caused by GPCR activation is directly related to the receptor number on cell surface. Using ACTOne assay, we were able to detect activities of some endogenous Gs coupled receptors in HEK293 cells that have not been reported in literature. In addition, we have also detected weak Gs coupled activity of a GPCR that was widely considered to be only linked to Gq coupled pathway. The ACTOne assay also provides a useful tool for GPCR de-orphanization.