5-HT5A Human Serotonin GPCR Cell Based Antagonist 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-HT5A receptors are widely present in the central nervous system but not or minimally in peripheral tissues. The 5-HT5A receptor class couples preferentially to GS to promote cAMP formation. Serotonin 5-HT5A receptor agonism may be hallucinatory and alter circadian rhythms.

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 β-galactosidase enzyme fragments (EA and PK). The resulting functional enzyme hydrolyzes substrate to generate a chemiluminescent signal.

Family:

GPCR

Sub Family:

Serotonin

Class:

Class A

Coupling:

Gi/Go

Protein Name:

5-HT5A

Uniprot Number:

P47898

Protein Aliases:

5-HT-5A|5-HT5A|Serotonin receptor 5A

Gene Name:

HTR5A

Gene ID:

3361

Gene Aliases:

5-HT5A

Accession Number:

NM_024012

Organism:

Human

Cell Type:

U2OS