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:

Full Length, Recombinant

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

GTPgammaS

Functional Mode:

Antagonist

Detection Method:

Radiometry

Measured Response:

Scintillation

Testing Information

Incubation:

45 min at 30°C

Control Inhibitor:

SB 242084

Criteria For Significance:

≥ 50% Increase in bound [35S]GTPgammaS relative to serotonin response, ≥ 50% Inhibition of serotonin-induced bound [35S]GTPgammaS

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:

16

Turnaround Time

Standard:

20 Business Days

Reference Compound Data

PubChem ID

3644637

Name

SB 242084

Measurement

0.0037μM - 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:

Taiwan - Taipei

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