AAV ACTOne Gi-GPCR Assay Kit-CB1

Cannabinoid Receptor 1 (CB1) is a type of G protein-coupled receptor (GPCR) that primarily binds to endocannabinoids, such as anandamide and 2-arachidonoylglycerol (2-AG), as well as to exogenous cannabinoids like THC (tetrahydrocannabinol) from cannabis. CB1 receptors are predominantly expressed in the central nervous system, especially in areas like the brain's cortex, hippocampus, basal ganglia, and cerebellum, but they are also found in peripheral tissues. CB1 is primarily coupled with the Gi/Go class of G proteins, which inhibit adenylate cyclase, leading to a reduction in cyclic AMP (cAMP) levels. Activation of CB1 receptors modulates neurotransmitter release, reducing the release of excitatory and inhibitory neurotransmitters in the brain. This modulation affects various physiological processes, including pain perception, appetite regulation, memory, mood, and motor function. Because of its role in these processes, CB1 is a significant target for therapeutic interventions in conditions such as chronic pain, epilepsy, obesity, and neurodegenerative diseases. However, its activation is also associated with psychoactive effects, making it a focus of research for both medical and recreational purposes.
This kit uses AAV vectors with a CMV promoter to co-express the CB1 and cyclic nucleotide-gated (CNG) channel, allowing researchers to conduct high-throughput screening and functional analysis of potential CB1-targeting compounds. The kit provides a sensitive and reliable method for evaluating the pharmacological properties of CB1 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.