AAV ACTOne Gi-GPCR Assay Kit-GALR1

Galanin Receptor 1 (GALR1) is a G protein-coupled receptor (GPCR) that binds to the neuropeptide galanin, which is involved in a variety of physiological processes, including modulation of pain, feeding behavior, mood regulation, and neuroendocrine functions. GALR1 is primarily coupled with the Gi/Go class of G proteins, which inhibits adenylate cyclase, leading to a reduction in cyclic AMP (cAMP) levels. This inhibition affects downstream signaling pathways that modulate neurotransmitter release and neuronal excitability. GALR1 is widely expressed in the central nervous system (CNS) and peripheral tissues, with high concentrations in the brain regions such as the hippocampus, hypothalamus, and spinal cord. These areas are associated with functions like memory, mood regulation, and pain perception. GALR1 is also expressed in various peripheral tissues, including the gastrointestinal tract and endocrine glands. The receptor has been implicated in several neurological and psychiatric conditions, including anxiety, depression, epilepsy, and Alzheimer's disease. Due to its role in pain modulation, GALR1 is also a target for research into new analgesic drugs. Additionally, GALR1's involvement in feeding behavior and metabolic regulation makes it a potential target for obesity and metabolic disorder treatments. The study of GALR1 continues to provide insights into the complex roles of galanin in the nervous system and holds promise for developing therapies for a range of disorders involving neuropeptide signaling.
This kit uses AAV vectors with a CMV promoter to co-express the GALR1 and cyclic nucleotide-gated (CNG) channel, allowing researchers to conduct high-throughput screening and functional analysis of potential GALR1-targeting compounds. The kit provides a sensitive and reliable method for evaluating the pharmacological properties of GALR1 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.