Biological Information

Background Information:

Histamine receptors belong to the superfamily of G protein-coupled seven transmembrane proteins. 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. Histamine receptors are found in most peripheral tissue and within the central nervous system. Histamine H3 receptors on nerve terminals function as feedback inhibitors in a wide variety of organ systems.

Family:

GPCR

Sub Family:

Histamine

Class:

Class A

Protein Name:

H3

Uniprot Number:

Q9Y5N1

Protein Aliases:

HH3R|G-protein coupled receptor 97

Gene Name:

HRH3

Gene ID:

11255

Gene Aliases:

GPCR97

Accession Number:

NM_007232

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]Nalpha -Me-histamine

Ligand Kd (nM):

0.32

Ligand Concentration:

1 nM

Non Specific:

1 µM (R)alpha -Me-histamine

Incubation:

60 min at RT

Control Inhibitor:

(R)-alpha-Methylhistamine

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

774

Name

Histamine

Measurement

5.9nM - IC50

PubChem ID

2756

Name

Cimetidine

Measurement

- IC50

PubChem ID

4992

Name

Pyrilamine

Measurement

53000nM - IC50

PubChem ID

156615

Name

(R)-alpha-Methylhistamine

Measurement

2.56nM - IC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Adverse / Beneficial Action:

Histamine H3 receptors are presynaptic receptors present on histaminergic nerve terminals in the CNS that exert feedback regulation of histamine synthesis and release.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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