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

Item: 307920

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OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

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+].

No. of Assays on Panel:

Assays on Panel:

Family

GPCR

Name

5-HT2B Human Serotonin GPCR Cell Based Agonist Proliferation LeadHunter Assay - TW

Item

307920-0

Protein

5-HT2B

Organism

Human

Assay Sub Type

Cell Based

Family

GPCR

Name

5-HT2B Human Serotonin GPCR Cell Based Antagonist Proliferation LeadHunter Assay - TW

Item

307920-1

Protein

5-HT2B

Organism

Human

Assay Sub Type

Cell Based

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

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist & Antagonist

Detection Method:

Luminescence

Measured Response:

Luminescence

Testing Information

Procedure Summary:

CHO-K1 cells expressing human recombinant 5HT2B receptors are seeded in modified DMEM (2 x 10⁴ cells/well) and incubated at 37°C 5% CO₂ incubator for 24 hours. Test compound and/or vehicle is incubated with cells at 37°C for 24 hours. After 24 hours, the luminescent reagent is then added for additional 10 minutes at room temperature. Luminescence is measured on the microplate reader. Test compound-induced stimulation of cell proliferation by 50 percent or more (≥50%), relative to 3 μM serotonin HCl control response, indicates significant agonist activity. Test compound-induced suppression of 50 nM serotonin HCl induced cell proliferation by 50 percent or more (≥50%) indicates significant antagonist activity.

Incubation:

1 d at 37°C

Control Inhibitor:

SB 206553

Control Activator:

Serotonin (5-HT)

Criteria For Significance:

≥ 50% Increase in proliferation relative to serotonin HCl response, ≥ 50% Inhibition of serotonin HCl-induced proliferation

Test Concentration / Dose:

Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM

Test Sample Requirements:

75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)

Minimum Order Quantity:

Turnaround Time

Standard:

20 Business Days

Reference Compound Data

PubChem ID

25102595

Name

SB-206553 HCl hydrate

Measurement

0.14μM - IC50

PubChem ID

160436

Name

Serotonin HCl

Measurement

0.011μM - EC50

Clinical Relevance

Therapeutic Area:

Cardiovascular

Adverse / Beneficial Action:

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.

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei