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
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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