AAV ACTOne Gs-GPCR Assay Kit-DRD1

The Dopamine Receptor D1 (DRD1) is a G protein-coupled receptor (GPCR) that is part of the D1-like family of dopamine receptors, which also includes the D5 receptor. DRD1 is primarily coupled with the Gs class of G proteins, which activate adenylate cyclase, leading to an increase in cyclic AMP (cAMP) levels. This receptor is widely expressed in the central nervous system, particularly in regions such as the striatum, where it plays a key role in regulating motor control, reward, and cognitive functions. DRD1 is involved in several physiological processes, including modulating the excitability of neurons, influencing synaptic plasticity, and regulating the release of other neurotransmitters. Dysregulation of DRD1 signaling has been implicated in various neurological and psychiatric disorders, including Parkinson's disease, schizophrenia, and drug addiction. Given its central role in dopaminergic signaling, DRD1 is a target for therapeutic research, particularly in the development of treatments for movement disorders and conditions involving dopaminergic dysfunction.
This kit uses AAV vectors with a CMV promoter to co-express the DRD1 and cyclic nucleotide-gated (CNG) channel, allowing researchers to conduct high-throughput screening and functional analysis of potential DRD1-targeting compounds. The kit provides a sensitive and reliable method for evaluating the pharmacological properties of DRD1 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.