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.

cAMP Hunter™ Gi cell lines overexpress naturally Gi coupled, wild type GPCRs and are designed to detect inhibition of intracellular cAMP production in response to agonist stimulation of the receptor. These cell lines are designed to be used in conjunction with the HitHunter® cAMP Assay Detection Kit.

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

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

PAM

Testing Information

Control Activator:

(R)-alpha-Methylhistamine

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 10 concentrations are selected

Test Sample Requirements:

40uL of a 1000X stock for the first assay and 2uL for each additional assay (assay = 1 target, 1 readout, 1 mode)

Minimum Order Quantity:

20

Turnaround Time

Standard:

15 Business Days

Clinical Relevance

Adverse / Beneficial Action:

Histamine H3 receptor agonism may impair memory acquisition and cause sedation, vasoldilation, bronchodilation, negative chronotropic activity and reduce gastrointestinal motilit

Additional Information

Brand:

LeadHunter

Testing Location:

USA - Fremont, CA