AAV ACTOne Gi-GPCR Assay Kit-GRM2

Metabotropic Glutamate Receptor 2 (GRM2) is a type of G protein-coupled receptor (GPCR) that belongs to the group II metabotropic glutamate receptors, which also includes GRM3. GRM2 is activated by the neurotransmitter glutamate, which is the primary excitatory neurotransmitter in the central nervous system. Unlike ionotropic glutamate receptors that directly mediate fast synaptic transmission, metabotropic receptors like GRM2 modulate neuronal activity indirectly through G protein signaling pathways. GRM2 is primarily coupled with the Gi/Go class of G proteins, which inhibit adenylate cyclase activity, leading to a reduction in cyclic AMP (cAMP) levels. This decrease in cAMP modulates several downstream signaling pathways, influencing neurotransmitter release, neuronal excitability, and synaptic plasticity. Specifically, GRM2 plays a role in reducing the release of glutamate and other neurotransmitters, helping to regulate excitatory transmission and maintain neuronal balance. Due to its regulatory role in glutamate signaling, GRM2 is a significant target for therapeutic research in a variety of neurological and psychiatric disorders, including schizophrenia, anxiety, depression, and neurodegenerative diseases. Modulating GRM2 activity with specific agonists or antagonists offers potential treatment strategies aimed at restoring normal glutamate levels and improving symptoms associated with these conditions.
This kit uses AAV vectors with a CMV promoter to co-express the GRM2 and cyclic nucleotide-gated (CNG) channel, allowing researchers to conduct high-throughput screening and functional analysis of potential GRM2-targeting compounds. The kit provides a sensitive and reliable method for evaluating the pharmacological properties of GRM2 drugs, such as agonists and antagonists, in a live-cell environment.

Please contact us at for specific academic pricing.

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.