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.

cAMP Hunter™ Gi cell lines overexpress naturally Gi coupled, wild type GPCRs and are designed to detect inhibition of intracellular cAMP production in response to agonist stimulation of the receptor. These cell lines are designed to be used in conjunction with the HitHunter® cAMP Assay Detection Kit.

Family:

GPCR

Sub Family:

Serotonin

Class:

Class A

Coupling:

Gi/Go

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_000524.2

Organism:

Human

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist

Testing Information

Control Activator:

serotonin

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 10 concentrations are selected

Test Sample Requirements:

40uL of a 1000X stock for the first assay and 2uL for each additional assay (assay = 1 target, 1 readout, 1 mode)

Minimum Order Quantity:

20

Turnaround Time

Standard:

15 Business Days

Clinical Relevance

Adverse / Beneficial Action:

Serotonin 5-HT1A receptor agonism may be antidepressant, anxiolytic, antipsychotic, reduce traumatic brain injury and emesis. Receptor antagonism may be anxiogenic and contribute to depression and suicide.

Additional Information

Brand:

LeadHunter

Testing Location:

USA - Fremont, CA