5-HT2B Human Serotonin GPCR [3H] LSD Binding Agonist Radioligand LeadHunter Assay - TW

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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-HT2B

Uniprot Number:

P41595

Protein Aliases:

5-HT2B|Serotonin receptor 2B

Gene Name:

HTR2B

Gene ID:

3357

Gene Aliases:

5-HT(2B)|5-HT2B

Accession Number:

NM_000867

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-HT₂ʙ receptor expressed in CHO-K1 cells are used to prepare membranes in modified Tris-HCl buffer pH 7.4. A 30 µg‡ aliquot of membrane protein is incubated with 1.2 nM [³H]LSD for 60 minutes at 37°C. Non-specific binding is estimated in the presence of 10 µM serotonin. Membranes are filtered and washed, the filters are then counted to determine [³H]LSD specifically bound. Compounds are screened at 10 µM.

Ligand:

[³H] Lysergic acid diethylamide (LSD)

Ligand Kd (nM):

2.1

Ligand Concentration:

1.2 nM

Non Specific:

10 µM Serotonin (5-HT)

Incubation:

60 min at 37°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:

10 Business Days

Reference Compound Data

PubChem ID

1683

Name

3-Tropanyl-3,5-dichlorobenzoate

Measurement

6μM - IC50

PubChem ID

2107

Name

Alpha-methyl-5-HT

Measurement

0.036μM - IC50

PubChem ID

3822

Name

Ketanserin

Measurement

0.84μM - IC50

PubChem ID

4106

Name

Methiothepin

Measurement

0.00065μM - IC50

PubChem ID

4946

Name

Propranolol

Measurement

0.38μM - IC50

PubChem ID

5074

Name

Ritanserin

Measurement

0.000026μM - IC50

PubChem ID

9681

Name

Methysergide

Measurement

0.00094μM - IC50

PubChem ID

28693

Name

Metergoline

Measurement

0.00088μM - IC50

PubChem ID

68848

Name

Mesulergine

Measurement

0.0063μM - IC50

Clinical Relevance

Therapeutic Area:

Cardiovascular

Adverse / Beneficial Action:

Serotonin 5-HT2B receptor agonism may facilitate pulmonary and peripheral hypertension. Receptor antagonism may be useful for the treatment of migraine headache.

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei