5-HT2A Human Serotonin GPCR Binding Antagonist Radioligand LeadHunter Assay - TW

Item: 271650

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OVERVIEW

DOCUMENTS/REFERENCES

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:

Full Length, Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometry

Measured Response:

Scintillation

Testing Information

Procedure Summary:

Human recombinant serotonin 5-HT₂ᴀ receptors expressed in CHO-K1 cells are used in modified Tris-HCl buffer pH 7.4. A 30 µg‡ aliquot is incubated with 1 nM [³H]Ketanserin for 60 minutes at 25°C. Non-specific binding is estimated in the presence of 1 µM Mianserin. Receptors are filtered and washed, the filters are then counted to determine [³H]Ketanserin specifically bound. Compounds are screened at 10 µM.

Ligand:

[³H] Ketanserin

Ligand Kd (nM):

0.2

Ligand Concentration:

1 nM

Non Specific:

1 µM Mianserin

Incubation:

60 min at 25°C

Control Inhibitor:

Ketanserin

Criteria For Significance:

≥ 50% of max stimulation or inhibition

Test Concentration / Dose:

Suggested concentration for initial testing is 10 uM

Test Sample Requirements:

Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).

Minimum Order Quantity:

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

1683

Name

3-Tropanyl-3,5-dichlorobenzoate

Measurement

>10μM - IC50

PubChem ID

3822

Name

Ketanserin

Measurement

0.00080μM - IC50

PubChem ID

24278124

Name

Serotonin (5-HT)

Measurement

0.58μM - 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:

Taiwan - Taipei