B1 Human Bradykinin GPCR Binding Antagonist Radioligand LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Bradykinin receptors 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. Bradykinin receptors are found in most peripheral tissue and within the central nervous system. Bradykinin B1 receptor agonism may result in cough, algesia, inflammation and vasodilation. Bradykinin B1 receptor antagonism may find therapeutic use in the treatment of chronic pain and inflammation.
Family:
GPCR
Sub Family:
Bradykinin
Class:
Class A
Protein Name:
B1
Uniprot Number:
P46663
Protein Aliases:
BK-1 receptor
Gene Name:
BDKRB1
Gene ID:
623
Gene Aliases:
BKR1|B1BKR|bradyb1
Organism:
Human
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometry
Measured Response:
Radiometric
Testing Information
Procedure Summary:
Human recombinant bradykinin B1 receptors expressed in CHO-K1 cells are used in modified HEPES buffer pH 7.4. A 0.044 mg* aliquot is incubated with 0.3 nM [³H]Kallidin[des-Arg10, Leu9] for 60 minutes at 25°C. Non-specific binding is estimated in the presence of 10 µM Des-Arg9- (Leu8)-Bradykinin. Membranes are filtered and washed, the filters are then counted to determine [³H]Kallidin[des-Arg10, Leu9] specifically bound. Compounds are screened at 10 µM. *Membrane protein may change from lot to lot, the concentration used will be adjusted if necessary.
Ligand:
[³H] (Des-Arg¹⁰, Leu⁹)- Kallidin
Ligand Kd (nM):
0.3
Ligand Concentration:
0.3 nM
Non Specific:
10 µM (Des-Arg⁹, Leu⁸)-Bradykinin
Incubation:
60 min at 25°C
Control Inhibitor:
Des-Arg¹⁰-Kallidin
Criteria For Significance:
≥ 50% of max stimulation or inhibition
Test Concentration / Dose:
Suggested concentration for initial testing is 10 uM
Minimum Order Quantity:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Inflammation/Allergy
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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