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:

Agonist

Detection Method:

Fluorimetry

Measured Response:

Fluorescence

Testing Information

Incubation:

RT

Control Activator:

NKB [MePhe7]

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

5079497

Name

Senktide

Measurement

0.79nM - EC50

PubChem ID

44338651

Name

[Sar9,Met(O2)11]-SP

Measurement

9nM - EC50

PubChem ID

57339975

Name

NKB [MePhe7]

Measurement

0.1nM - EC50

PubChem ID

Name

[Nleu10]-NKA (4-10)

Measurement

216nM - EC50

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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