Biological Information
Background Information:
GABA is the major inhibitory transmitter in the mammallian central nervous system. GABAB 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. GABAB receptors are located on pre- and postsynaptic neurones in the central nervous system and peripheral autonomic nerve fibers and sensory fibers.
Family:
GPCR
Sub Family:
GABAB
Class:
Class C
Protein Name:
GABAB (B1/B2)
Uniprot Number:
Q9UBS5
Protein Aliases:
GABA-B receptor
Gene Name:
GABBR1
Gene ID:
2550
Gene Aliases:
hGB1a|GPRC3A
Accession Number:
XM_017007985
Organism:
Human
Construct Details:
Full Length, Recombinant
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Antagonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Incubation:
20 min at 37°C
Control Inhibitor:
CGP 54626
Criteria For Significance:
≥50% decrease in cAMP relative to SKF 97541 response, ≥50% Inhibition of SKF 97541-induced cAMP decrease
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
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
RELATED SOLUTIONS