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:

NK3

Uniprot Number:

P29371

Protein Aliases:

neurokinin beta receptor

Gene Name:

TACR3

Gene ID:

6870

Gene Aliases:

NK3R|TAC3R

Accession Number:

NM_001059

Organism:

Human

Construct Details:

Recombinant

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

Fluorimetry

Measured Response:

Fluorescence

Testing Information

Incubation:

RT

Control Inhibitor:

SB 222200

Control Activator:

[MePhe7]-NKB (1 nM)

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.

Test Sample Requirements:

Minimum for 1) Screen: 70 µL of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM finµL 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:

16

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

104974

Name

Saredutant

Measurement

2800nM - IC50

PubChem ID

6604009

Name

SB 222200

Measurement

24nM - IC50

PubChem ID

16131028

Name

spantide II

Measurement

7100nM - IC50

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:

France - Celle L'Evescault

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