5-HT2C Human Serotonin GPCR Cell Based Agonist Arrestin 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-HT2C 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. Activation of the GPCR-PK induces β-Arrestin-EA recruitment, forcing complementation of the two enzyme fragments. The resulting functional enzyme hydrolyzes substrate to generate a chemiluminescent signal. PathHunter cell lines expressing Gq-coupled receptors can also be used to detect calcium mobilization.

Family:

GPCR

Sub Family:

Serotonin

Class:

Class A

Coupling:

Gq

Protein Name:

5-HT2C

Uniprot Number:

P28335

Protein Aliases:

5-HT2C|5-HTR2C|5-hydroxytryptamine receptor 1C|5-HT-1C|5-HT1C|Serotonin receptor 2C

Gene Name:

HTR2C

Gene ID:

3358

Gene Aliases:

5-HT2C|5HTR2C

Accession Number:

NM_000868.2

Organism:

Human

Cell Type:

U2OS