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-HT6 receptors are present in the central nervous system but not or minimally in peripheral tissues. The 5-HT6 receptor class couples preferentially to GS to promote cAMP formation.

Family:

GPCR

Sub Family:

Serotonin

Class:

Class A

Protein Name:

5-HT6

Uniprot Number:

P50406

Protein Aliases:

5-HT6|Serotonin receptor 6

Gene Name:

HTR6

Gene ID:

3362

Gene Aliases:

5-HT6|5-HT6R

Accession Number:

NM_000871

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]LSD

Ligand Kd (nM):

1.8

Ligand Concentration:

2 nM

Non Specific:

100 µM Serotonin

Incubation:

120 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

- IC50

PubChem ID

4106

Name

Methiothepin

Measurement

1.2nM - IC50

PubChem ID

5202

Name

serotonin

Measurement

150nM - IC50

PubChem ID

Name

MDL72222

Measurement

- IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

Serotonin 5-HT6 receptor agonism may improve learning and memory disorders. Receptor antagonism may be useful in the treatment of depression, schizophrenic disorders and associated aggressive behaviors.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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