Application

Human 5-HT2A GPCR frozen cells for Calcium Flux FLIPR Assays.

Biochem/physiol Actions

GPCR Class: A Protein Target: 5-HT2A Target Sub-Family: Serotonin

Cell Line Description

GPCR Cell Lines Host cells: Chem-1

Components

Pack contains 2 vials of mycoplasma-free cells, 1 ml per vial.Fifty (50) mL of Media Component.

Disclaimer

This product contains genetically modified organisms (GMO). Within the EU GMOs are regulated by Directives 2001/18/EC and 2009/41/EC of the European Parliament and of the Council and their national implementation in the member States respectively.

General description

Millipore’;s Ready-to-Assay GPCR frozen cells are designed for simple, rapid calcium assays with no requirement for intensive cell culturing. Millipore has optimized the freezing conditions to provide cells with high viability and functionality post-thaw. The user simply thaws the cells and resuspends them in media, dispenses cell suspension into assay plates and, following over night recovery, assays for calcium response.

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-HT2A, which couples to Gq/11 to increase intracellular calcium, is widely expressed at central and peripheral sites of 5-HT action, and contributes to many of the physiological effects of 5-HT. The hallucinogenic activity of LSD is mediated in part by its action as an partial to full agonist at 5-HT2A, and the activity of atypical antipsychotics such as clozapine appears to be mediated in part by antagonism of 5-HT2A (Barnes and Sharp, 1999). Millipore’;s cloned human 5-HT2A -expressing cell line is made in the Chem-1 host, which supports high levels of recombinant 5-HT2A expression on the cell surface for functional detection via the calcium signaling pathway. Thus, the cell line is an ideal tool for screening for agonists, antagonists and modulators at 5-HT2A.