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-HT7 receptors are present in the central nervous system and peripheral tissues. The 5-HT7 receptor class couples preferentially to GS to promote cAMP formation.

Family:

GPCR

Sub Family:

Serotonin

Class:

Class A

Protein Name:

5-HT7

Uniprot Number:

P34969

Protein Aliases:

5-HT7|5-HT-X|Serotonin receptor 7

Gene Name:

HTR7

Gene ID:

3363

Gene Aliases:

5-HT7

Accession Number:

NM_000872

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]LSD

Ligand Kd (nM):

2.3

Ligand Concentration:

4 nM

Non Specific:

10 µM Serotonin

Incubation:

120 min at RT

Control Inhibitor:

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 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

53nM - IC50

PubChem ID

1683

Name

3-Tropanyl-3,5-dichlorobenzoate

Measurement

- IC50

PubChem ID

3822

Name

Ketanserin

Measurement

74nM - IC50

PubChem ID

5202

Name

serotonin

Measurement

0.45nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

Serotonin 5-HT7 receptor agonism may alter circadian rhythms and cause arterial vasodilation. Receptor antagonism may be useful in the treatment of migraine and irritable bowel syndrome.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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