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

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]mesulergine

Ligand Kd (nM):

0.5

Ligand Concentration:

1 nM

Non Specific:

10 µM RS 102221

Incubation:

120 min at 37°C

Control Inhibitor:

RS-102221

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 final 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:

2

Turnaround Time

Standard:

10 Business Days

Reference Compound Data

PubChem ID

3822

Name

Ketanserin

Measurement

216nM - IC50

PubChem ID

5202

Name

serotonin

Measurement

31nM - IC50

PubChem ID

3045227

Name

Ro-600175

Measurement

19nM - IC50

PubChem ID

3693566

Name

RS-102221

Measurement

3.1nM - 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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