Biological Information

Background Information:

Tachykinins 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. Tachykinin receptors are found in most peripheral tissue and within the central nervous system. Tachykinin receptor agonism may result in vasodilation, salivary and mucous secretion, emesis, brochoconstriction, micturation, modulate behavior, increase pain transmission and neurogenic inflammation.

PathHunter Activated GPCR Internalization cell lines are engineered to co-express an untagged GPCR, Enzyme Acceptor (EA) tagged β-Arrestin, and a ProLink™ (PK) tag localized to the endosomes. Activation of the GPCR induces β-Arrestin recruitment, followed by internalization of the Receptor/Arrestin-EA complex in PK-tagged endosomes. This forces complementation of the two β-galactosidase enzyme fragments (EA and PK), forming functional enzyme that hydrolyzes substrate to generate a chemiluminescent signal.

Family:

GPCR

Sub Family:

Tachykinin

Class:

Class A

Coupling:

Gq

Protein Name:

NK2

Uniprot Number:

P21452

Protein Aliases:

NK-2 receptor|NK-2R|Neurokinin A receptor|Tachykinin receptor 2

Gene Name:

TACR2

Gene ID:

6865

Gene Aliases:

SKR|NK2R|NKNAR|TAC2R

Accession Number:

AY322545

Organism:

Human

Cell Type:

U2OS

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

β-Arrestin Isoform:

β-Arrestin-2

Testing Information

Control Inhibitor:

GR 159897

Control Activator:

Substance P

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:

Tachykinin receptor antagonism may find therapeutic use in the treatment of pain, emesis, inflammatory diseases and anxiety or depression.

Additional Information

Brand:

LeadHunter

Testing Location:

USA - Fremont, CA