AAV ACTOne Gi-GPCR Assay Kit-OPRK1

OPRK1, also known as the κ-Opioid Receptor (KOR), is a G protein-coupled receptor (GPCR) that is part of the opioid receptor family, which also includes the mu (MOR) and delta (DOR) opioid receptors. The OPRK1 receptor is activated by endogenous ligands such as dynorphins, which are peptides that play a critical role in the body's response to stress, pain, and emotion. When activated, OPRK1 is primarily coupled with the Gi/Go class of G proteins, leading to inhibition of adenylate cyclase, a reduction in cyclic AMP (cAMP) levels, and modulation of ion channels, which collectively result in decreased neuronal excitability. This receptor is involved in a wide range of physiological functions, including pain modulation, stress response, mood regulation, and consciousness. Activation of OPRK1 generally produces analgesia, but it is also associated with dysphoria, sedation, and aversive effects, which differentiate it from the euphoric effects typically produced by activation of the mu-opioid receptor (MOR). Because of these properties, OPRK1 is a target of interest in the development of new pain therapies that aim to avoid the addictive potential of traditional opioids. Additionally, OPRK1 is being studied for its role in stress, depression, and substance abuse disorders, as modulating this receptor may provide therapeutic benefits in these areas. Researchers are exploring both agonists and antagonists of OPRK1 to better understand its potential in treating various conditions related to pain, mood, and addiction.
This kit uses AAV vectors with a CMV promoter to co-express the OPRK1 and cyclic nucleotide-gated (CNG) channel, allowing researchers to conduct high-throughput screening and functional analysis of potential OPRK1-targeting compounds. The kit provides a sensitive and reliable method for evaluating the pharmacological properties of OPRK1 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.