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-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+].

Family:

GPCR

Sub Family:

Serotonin

Class:

Class A

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

Organism:

Human

Construct Details:

Recombinant

Cell Type:

HEK293

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

HTRF

Testing Information

Incubation:

30 min at 37°C

Control Inhibitor:

SB 206553

Control Activator:

serotonin (10 nM)

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.

Test Sample Requirements:

Minimum for 1) Screen: 60 µL of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM finµL testing. 2) Dose Response: 90 µL of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM.

Minimum Order Quantity:

16

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

3822

Name

Ketanserin

Measurement

750nM - IC50

PubChem ID

5163

Name

SB 206553

Measurement

9.4nM - IC50

PubChem ID

68848

Name

Mesulergine

Measurement

11nM - IC50

PubChem ID

3277600

Name

SB 204741

Measurement

3330nM - IC50

Clinical Relevance

Therapeutic Area:

Metabolic Diseases

Adverse / Beneficial Action:

Serotonin5-HT2C receptorantagonism may lead to obesity and increased tendency to spontaneous clonic seizures.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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