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

PubChem ID

1220

Name

8-OH-DPAT

Measurement

200000nM - Ic50

PubChem ID

3822

Name

Ketanserin

Measurement

30000nM - IC50

PubChem ID

5202

Name

serotonin

Measurement

170nM - IC50

PubChem ID

119376

Name

GR 113808

Measurement

0.6nM - IC50

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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