5-HT2A Mouse Serotonin GPCR Cell Based Antagonist Calcium Flux (in Arrestin Cell Line) LeadHunter Assay - US

Background Information:

Serotonin 5-HT receptors belong to the superfamily of G protein-coupled seven transmembrane proteins with the exception of the 5-HT3 subtype, which belongs to the ligand gated cation superfamily of receptors. G-protein-coupled receptors constitute one of the major signal transduction systems in eukaryotic cells. Coding sequences for these receptors, in those regions believed to contribute to the agonist-antagonist binding site, are strongly conserved across mammalian species. Serotonin 5-HT2 receptors are widely distributed in the central nervous system and peripheral tissues. The 5-HT2 receptor class couples preferentially to Gq/G11 to increase hydrolysis of inositol phosphates and elevate cytosolic [Ca2+]. PathHunter β-Arrestin GPCR cell lines are engineered to co-express the ProLink™ (PK) tagged GPCR and the Enzyme Acceptor (EA) tagged β-Arrestin. Calcium mobilization in PathHunter β-Arrestin GPCR cell lines expressing Gq-coupled GPCRs is monitored using a calcium sensitive dye that is loaded into cells. The esterified (inactive) calcium dye (probe) penetrates the cell membrane and becomes active after binding to intracellular calcium. Ligand binding stimulates GPCR activation, resulting in release of intracellular calcium stores from the ER, which leads to an increase in fluorescence in the presence of the activated calcium dye.

Family:

GPCR

Sub Family:

Serotonin

Class:

Class A

Coupling:

Gi/Go

Protein Name:

5-HT2A

Uniprot Number:

P35363

Protein Aliases:

5-hydroxytryptamine receptor 2A|5-HT-2A|Serotonin receptor 2A

Gene Name:

HTR2A

Gene ID:

15558

Gene Aliases:

HTR2|5-HT2A

Accession Number:

NM_172812

Organism:

Mouse

Cell Type:

CHO-K1