AAV ACTOne Gi-GPCR Assay Kit-DRD2

The Dopamine Receptor D2 (DRD2) is a G protein-coupled receptor (GPCR) that is part of the D2-like family of dopamine receptors, which also includes D3 and D4 receptors. DRD2 is primarily associated with the Gi/Go class of G proteins, which inhibit adenylate cyclase, leading to a reduction in cyclic AMP (cAMP) levels within the cell. This decrease in cAMP affects various intracellular signaling pathways, influencing neuronal excitability, neurotransmitter release, and synaptic plasticity. DRD2 is highly expressed in the central nervous system, particularly in the basal ganglia, a brain region involved in coordinating movement, reward, and cognitive functions. DRD2 plays a pivotal role in several physiological processes, and dysregulation of this receptor is associated with various neurological and psychiatric disorders. In Parkinson's disease, the loss of dopaminergic neurons reduces DRD2 activity, contributing to motor symptoms such as tremors and rigidity. In schizophrenia, overactivation of DRD2 is linked to positive symptoms like hallucinations and delusions. As a result, DRD2 is a key target for antipsychotic drugs, which often work by antagonizing this receptor to alleviate symptoms of schizophrenia. Conversely, dopaminergic agonists targeting DRD2 are used in treating Parkinson's disease to improve motor function. Given its central role in dopaminergic signaling, DRD2 continues to be a focal point for research aimed at understanding and treating a wide range of conditions involving dopamine dysregulation.
This kit uses AAV vectors with a CMV promoter to co-express the DRD2 and cyclic nucleotide-gated (CNG) channel, allowing researchers to conduct high-throughput screening and functional analysis of potential DRD2-targeting compounds. The kit provides a sensitive and reliable method for evaluating the pharmacological properties of DRD2 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.