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. The 5-HT1 receptor class couples preferentially to Gi/Go to inhibit cAMP formation. Serotonin 5-HT1A receptors are widely distributed in the central nervous system as well as in the periphery.

Family:

GPCR

Sub Family:

Serotonin

Class:

Class A

Protein Name:

5-HT1A

Uniprot Number:

P08908

Protein Aliases:

5-HT1A|G-21|Serotonin receptor 1A

Gene Name:

HTR1A

Gene ID:

3350

Gene Aliases:

ADRB2RL1|ADRBRL1

Organism:

Human

Construct Details:

Recombinant

Cell Type:

BA/F3

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

Fluorimetry

Measured Response:

Fluorescence

Testing Information

Incubation:

RT

Control Inhibitor:

(S)-WAY-100635

Control Activator:

Serotonine (15 nM)

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.

Test Sample Requirements:

Minimum for 1) Screen: 70 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

PubChem ID

24278121

Name

Ketanserine

Measurement

- IC50

PubChem ID

24278113

Name

(S)-WAY-100635

Measurement

1.95nM - IC50

PubChem ID

375975533

Name

MDL72222

Measurement

- IC50

PubChem ID

24277909

Name

Spiperone

Measurement

- IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

Serotonin 5-HT1A receptor agonists may be useful for the treatment of anxiety and depression.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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