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-HT2 receptors are widely distributed in the central nervous system and peripheral tissues. The 5-HT2 receptor class couples preferentially to Gq/G11 to increase hydrolysis of inositol phosphates and elevate cytosolic [Ca2+].

Family:

GPCR

Sub Family:

Serotonin

Class:

Class A

Protein Name:

5-HT2A

Uniprot Number:

P28223

Protein Aliases:

5-HT-2A|Serotonin receptor 2A

Gene Name:

HTR2A

Gene ID:

3356

Gene Aliases:

HTR2

Accession Number:

NM_000621

Organism:

Human

Construct Details:

Recombinant

Cell Type:

HEK293

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist

Detection Method:

HTRF

Testing Information

Incubation:

30 min at 37°C

Control Activator:

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 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

1833

Name

5-methoxytryptamine

Measurement

14nM - EC50

PubChem ID

5202

Name

serotonin

Measurement

25nM - EC50

PubChem ID

170617

Name

DOI

Measurement

5nM - EC50

PubChem ID

5311036

Name

BW 723C86

Measurement

410nM - EC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

Serotonin 5-HT2A receptor agonism may be hallucinogenic, facilitate vasoconstriction and gastrointestinal transit. Receptor antagonism may prevent peripheral vascular thrombosis, reduce psychosis and extrapyramidal side effects of antipsychotic agents.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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