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

Accession Number:

NM_000524

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]8-OH-DPAT

Ligand Kd (nM):

0.5

Ligand Concentration:

0.5 nM

Non Specific:

10 µM 8-OH-DPAT

Incubation:

60 min at RT

Control Inhibitor:

8-OH-DPAT

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

0.6nM - IC50

PubChem ID

3822

Name

Ketanserin

Measurement

2400nM - IC50

PubChem ID

5202

Name

serotonin

Measurement

1.8nM - IC50

PubChem ID

Name

MDL72222

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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