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.
Family:
GPCR
Sub Family:
Tachykinin
Class:
Class A
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:
NM_001057
Organism:
Human
Construct Details:
Full Length, Recombinant
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Agonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Incubation:
30 min at 37°C
Control Activator:
GR 64349
Criteria For Significance:
≥ 50% increase in IP-one relative to GR 64349 response, ≥ 50% Inhibition of GR 64349-induced response
Test Concentration / Dose:
Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM
Test Sample Requirements:
75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)
Minimum Order Quantity:
16
Turnaround Time
Standard:
20 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
Adverse / Beneficial Action:
Tachykinin receptor agonism may result in vasodilation, salivary and mucous secretion, emesis, brochoconstriction, micturation, modulate behavior, increase pain transmission and neurogenic inflammation. 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:
Taiwan - Taipei
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