H2 Human Histamine GPCR Binding Antagonist Radioligand LeadHunter Assay - FR

Item: 1208

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OVERVIEW

DOCUMENTS/REFERENCES

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.

Family:

GPCR

Sub Family:

Histamine

Class:

Class A

Protein Name:

Uniprot Number:

P25021

Protein Aliases:

HH2R|Gastric receptor I

Gene Name:

HRH2

Gene ID:

3274

Accession Number:

XM_005265904

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[125I]APT

Ligand Kd (nM):

2.9

Ligand Concentration:

0.075 nM

Non Specific:

100 µM Tiotidine

Incubation:

120 min at RT

Control Inhibitor:

Cimetidine

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:

Turnaround Time

Standard:

10 Business Days

Reference Compound Data

PubChem ID

774

Name

Histamine

Measurement

44000nM - IC50

PubChem ID

2756

Name

Cimetidine

Measurement

472nM - IC50

PubChem ID

4992

Name

Pyrilamine

Measurement

55000nM - IC50

PubChem ID

3001055

Name

Ranitidine

Measurement

69nM - IC50

Clinical Relevance

Therapeutic Area:

Gastroenterology

Adverse / Beneficial Action:

Histamine H2 receptor antagonism is used primarily in the treatment of peptic ulcers and gastroeosophageal reflux disease (GERD); reduction of gastric acid secretion may alter bioavailability and rate of absorption of some therapeutic agents.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault