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

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]ketanserin

Ligand Kd (nM):

0.6

Ligand Concentration:

0.5 nM

Non Specific:

1 µM Ketanserin

Incubation:

60 min at RT

Control Inhibitor:

Kétansérine

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

24278121

Name

kétansérine

Measurement

1.1nM - IC50

PubChem ID

57654276

Name

8OHDPAT

Measurement

15165nM - IC50

PubChem ID

24278124

Name

Sérotonine

Measurement

505nM - IC50

PubChem ID

671690

Name

MDL72222

Measurement

13260nM - IC50

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

RELATED SOLUTIONS

Item: 471
Item: 3196
Item: 3198
Item: G181
Item: P1
Item: P3