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-HT4 receptors are widely distributed in the central nervous system and peripheral tissues. The 5-HT4 receptor class couples preferentially to GS to promote cAMP formation.
Family:
GPCR
Sub Family:
Serotonin
Class:
Class A
Protein Name:
5-HT4
Uniprot Number:
Q13639
Gene Name:
HTR4
Gene ID:
3360
Gene Aliases:
5-HT4
Accession Number:
NM_000870
Organism:
Human
Construct Details:
Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Ligand:
[3H]GR 113808
Ligand Kd (nM):
0.15
Ligand Concentration:
0.3 nM
Non Specific:
100 µM Serotonin
Incubation:
60 min at 37°C
Control Inhibitor:
serotonin
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
Clinical Relevance
Therapeutic Area:
Gastroenterology
Adverse / Beneficial Action:
Serotonin 5-HT4 receptor agonism may facilitate mechanical intestinal allodynia. Receptor antagonism may be useful in the treatment of irritable bowel syndrome and cardiac arrhythmias.
Additional Information
Brand:
LeadHunter
Testing Location:
France - Celle L'Evescault
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