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