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:

Agonist

Detection Method:

Fluorimetry

Measured Response:

Fluorescence

Testing Information

Incubation:

RT

Control Activator:

Histamine

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

774

Name

Histamine

Measurement

47nM - EC50

PubChem ID

3077

Name

Dimaprit

Measurement

- EC50

PubChem ID

6054

Name

2-PHENYLETHANOL

Measurement

2500nM - EC50

PubChem ID

Name

R-alpha -Me-histamine

Measurement

- EC50

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

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