AAV ACTOne Gs-GPCR Assay Kit-HTR6

The Serotonin Receptor 6, HTR6, or 5-HT6 receptor, is a G protein-coupled receptor (GPCR) that primarily binds to serotonin (5-hydroxytryptamine, 5-HT). It is mainly expressed in the central nervous system, particularly in brain regions associated with cognition, learning, and memory, such as the cortex, hippocampus, and striatum. The HTR6 receptor is coupled with the Gs protein, which activates adenylate cyclase and increases cyclic AMP (cAMP) levels. Due to its involvement in cognitive processes, it is a target for drugs aimed at treating Alzheimer's disease, schizophrenia, and other cognitive disorders.
Family
Type
Mechanism
Potential
5-HT1
Gi/Go-protein coupled.
Decreasing cellular levels of cAMP.
Inhibitory
5-HT2
Gq/G11-protein coupled.
Increasing cellular levels of IP3 and DAG.
Excitatory
5-HT3
Ligand-gated Na+ and K+ cation channel.
Depolarizing plasma membrane.
Excitatory
5-HT4
Gs-protein coupled.
Increasing cellular levels of cAMP.
Excitatory
5-HT5
Gi/Go-protein coupled.
Decreasing cellular levels of cAMP.
Inhibitory
5-HT6
Gs-protein coupled.
Increasing cellular levels of cAMP.
Excitatory
5-HT7
Gs-protein coupled.
Increasing cellular levels of cAMP.
Excitatory
This kit uses AAV vectors with a CMV promoter to co-express the HTR6 and cyclic nucleotide-gated (CNG) channel, allowing researchers to conduct high-throughput screening and functional analysis of potential HTR6-targeting compounds. The kit provides a sensitive and reliable method for evaluating the pharmacological properties of HTR6 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.