AAV ACTOne Gi-GPCR Assay Kit-DRD3

The Dopamine Receptor D3 (D3R) is a type of G protein-coupled receptor (GPCR) that primarily binds dopamine, a neurotransmitter that plays a critical role in the brain's reward, motivation, and movement pathways. The D3 receptor is part of the D2-like receptor family, which also includes D2 and D4 receptors. It is predominantly coupled with the Gi/Go class of G proteins, which inhibit adenylate cyclase, leading to a reduction in cyclic AMP (cAMP) levels within the cell. D3 receptors are primarily found in regions of the brain associated with cognition, emotion, and reward, such as the limbic system. Because of their location and function, D3 receptors are implicated in various neurological and psychiatric disorders, including schizophrenia, addiction, and Parkinson's disease. Due to its role in modulating behavior and emotion, the D3 receptor is a target of interest for the development of drugs aimed at treating these conditions
This kit uses AAV vectors with a CMV promoter to co-express the DRD3 and cyclic nucleotide-gated (CNG) channel, allowing researchers to conduct high-throughput screening and functional analysis of potential DRD3-targeting compounds. The kit provides a sensitive and reliable method for evaluating the pharmacological properties of DRD3 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.