5-HT2B Human Serotonin GPCR Cell Based Agonist & Antagonist IP1 LeadHunter Assay - TW

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 5HT₂ʙ 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 hypertrophy in rodents. Receptor antagonism may be useful for the treatment of migraine headache.

No. of Assays on Panel:

2

Family:

GPCR

Sub Family:

Serotonin

Class:

Class A

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

Organism:

Human

Construct Details:

Full Length, Recombinant

Cell Type:

CHO-K1