5-HT2B Human Serotonin GPCR Cell Based Agonist Calcium Flux Assay (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+]. Agonists of the 5HT2B receptor stimulate heart valve cell growth leading to cardiac valvulopathy and primary pulmonary hypertension. Antagonists prevent primary pulmonary hypertension and have been shown to prevent agonist-induced heart hyperthrophy in rodents. Receptor antagonism may be useful for the treatment of migraine headache.

DiscoverX® Calcium cell lines overexpress naturally Gq coupled, wildtype GPCRs and are designed to detect calcium mobilization in response to agonist stimulation of the receptor. Signal can be detected using the Calcium No WashPLUS Detection Kit.

Family:

GPCR

Sub Family:

Serotonin

Class:

Class A

Coupling:

Gq

Protein Name:

5-HT2B

Uniprot Number:

P41595

Protein Aliases:

5-HT2B|Serotonin receptor 2B

Gene Name:

HTR2B

Gene ID:

3357

Gene Aliases:

5-HT(2B)|5-HT2B

Accession Number:

NM_000867.4

Organism:

Human

Cell Type:

HEK293