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:
NK1
Uniprot Number:
P25103
Protein Aliases:
NK-1 receptor|NK-1R|Tachykinin receptor 1
Gene Name:
TACR1
Gene ID:
6869
Gene Aliases:
SPR|NK1R|NKIR|TAC1R
Accession Number:
NM_001058
Organism:
Human
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Ligand:
[125I]-Substance P LYS3
Ligand Kd (nM):
0.04
Ligand Concentration:
0.05 nM
Non Specific:
1 µM [Sar9,Met(O2)11]-SP
Incubation:
30 min at RT
Control Inhibitor:
[Sar9,Met(O2)11]-SP
Test Concentration / Dose:
Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.
Test Sample Requirements:
Minimum for 1) Screen: 60 µl of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM final 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:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
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:
France - Celle L'Evescault
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