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. Serotonin 5-HT3 receptors appear to be present exclusively in neural tissue. Serotonin 5-HT3 receptor agonism may reduce water intake, cause hyperglycemia, facilitate gastric emptying and emesis. Receptor antagonism may prevent nausea and vomiting induced by cancer chemotherapy, diarrhea-predominant IBS and cause headache.

Family:

Ion Channel

Sub Family:

Serotonin

Class:

Ligand-Gated

Protein Name:

5-HT3A

Uniprot Number:

P46098

Gene Name:

HTR3A

Gene ID:

3359

Gene Aliases:

5HT3R,HTR3

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]BRL 43694

Ligand Kd (nM):

1.15

Ligand Concentration:

0.5 nM

Non Specific:

10 µM MDL 72222

Incubation:

120 min at RT

Control Inhibitor:

3-Tropanyl-3,5-dichlorobenzoate

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

1220

Name

8-OH-DPAT

Measurement

103000nM - iC50

PubChem ID

1683

Name

3-Tropanyl-3,5-dichlorobenzoate

Measurement

10nM - iC50

PubChem ID

3696

Name

Imipramine

Measurement

nM - iC50

PubChem ID

5202

Name

serotonin

Measurement

690nM - iC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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