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:

H1

Uniprot Number:

P35367

Protein Aliases:

HH1R

Gene Name:

HRH1

Gene ID:

3269

Accession Number:

XM_017006283

Organism:

Human

Construct Details:

Recombinant

Cell Type:

HEK293

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

Fluorimetry

Measured Response:

Fluorescence

Testing Information

Incubation:

RT

Control Inhibitor:

Pyrilamine

Control Activator:

histamine (300 nM)

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.

Test Sample Requirements:

Minimum for 1) Screen: 70 µL of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM finµL 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:

16

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

2756

Name

Cimetidine

Measurement

- IC50

PubChem ID

2790

Name

Clobenpropit

Measurement

- IC50

PubChem ID

4992

Name

Pyrilamine

Measurement

6nM - IC50

PubChem ID

5282443

Name

triprolidine

Measurement

13nM - IC50

Clinical Relevance

Therapeutic Area:

Inflammation/Allergy

Adverse / Beneficial Action:

Histamine H1 receptor antagonism is used in the treatment of various immediate hypersensitivity reactions; action upon the central nervous system may cause sedation while high doses may result in convulsions, especially in infants.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

RELATED SOLUTIONS

Item: 870
Item: 2542
Item: G115
Item: P347
Item: P460-EU
Item: P452-EU