ChemiScreen™ 5-HT2C Serotonin Receptor Stable Cell Line

5-Hydroxytryptamine (5-HT, also commonly known as serotonin) is synthesized in enterochromaffin cells in the intestine and in serotonergic nerve terminals. In the periphery, 5-HT mediates gastrointestinal motility, platelet aggregation, and contraction of blood vessels. Many functions of the central nervous system are influenced by 5-HT, including sleep, motor activity, sensory perception, arousal and appetite. A family of 12 GPCRs and one ion channel mediate the biological effects of 5-HT (Hoyer et al., 1994). 5-HT2C, which couples to Gq in most cells to stimulate intracellular calcium, is prominently expressed in brain and appears to modulate depression, anxiety and appetite (Miller, 2005; Serretti et al., 2004; Wood, 2003). The mRNA encoding 5-HT2C undergoes selective RNA editing that changes 4 amino acids in the second intracellular loop; these changes result in alteration of efficiency of coupling to G proteins. Alterations in editing of 5-HT2C have been detected in victims of suicidal depression and in mice treated with the SSRI, fluoxetine (Tohda et al., 2006). The cloned human 5-HT2C -expressing cell line is made in the Chem-1 host, which supports high levels of recombinant 5-HT2C expression on the cell surface and contains high levels of the promiscuous G protein Gα15 to couple the receptor to the calcium signaling pathway. Thus, the cell line is an ideal tool for screening for antagonists of interactions between 5-HT2C and its ligands.

Catalog No. Size Price Quantity
HTS132C 2 Vials $9,389.00

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Application
Calcium Flux Assay
Family
5-Hydroxytryptamine (Serotonin)
Target
5HT2C
Accession Number
NM_000868
Species
Human
Host Cell Type
Chem-1
Content
2 Vials of mycoplasma-free cells, 1 ml per vial
Storage
Cell vials are to be stored in the vapor phase of liquid N2.
  • [User Manual] ChemiSCREEN™ and ChemiBRITE™ Cell Lines

    The ChemiSCREEN and ChemiBRITE Cell Lines are designed to enable the measurement of intracellular calcium levels when a GPCR of interest has been activated by a ligand. These cell lines are suitable for studying small molecules as well as biologics. The assay protocol has been optimized for use in either a 384-well or 96-well format.

    ChemiSCREEN and ChemiBRITE cells stably expres...

    [User Manual] ChemiSCREEN™ and ChemiBRITE™ Cell Lines