Biological Information
Background Information:
GABA is the major inhibitory transmitter in the mammalian 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 neurons in the central nervous system and peripheral autonomic nerve fibers and sensory fibers. At least two GABAB1 receptor isoforms exist. Functional GABAB receptors are heterodimerized by GABAB1 and GABAB2 subunits. GABAB1a/B2 receptor agonism is useful in the treatment of spasticity and may be anxiolytic, anticonvulsant, muscle relaxation, antihyperalgesic effect, cause sedation and impair motor function. Receptor antagonism may cause convulsions.
No. of Assays on Panel:
2
Assays on Panel:
Family
GPCR
Name
GABAB (B1/B2) Human GABAB GPCR Cell Based Agonist cAMP LeadHunter Assay - TW
Item
312600-0
Protein
GABAB (B1/B2)
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
GABAB (B1/B2) Human GABAB GPCR Cell Based Antagonist cAMP LeadHunter Assay - TW
Item
312600-1
Protein
GABAB (B1/B2)
Organism
Human
Assay Sub Type
Cell Based
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:
Agonist & Antagonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Procedure Summary:
Human recombinant GABAB1A/B2 receptors expressed in CHO-K1 cells are used. Test compound and/or vehicle is incubated with the cells (2 x 10^5 /ml) in incubation buffer for 20 minutes at 37°C. Test compound-induced decrease of cAMP by 50 percent or more (≥50%) relative to the 10 μM SKF 97541 response indicates possible GABAB1A/B2 receptor agonist activity. Test compound-induced inhibition of 0.2 μM SKF 97541-induced decrease of cAMP response by 50 percent or more (≥50%) indicates receptor antagonist activity.
Incubation:
20 min at 37°C
Control Inhibitor:
CGP 54626
Control Activator:
SKF 97541
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
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