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. GABAB receptor agonism is useful in the treatment of spasticity and may be anxiolytic, anticonvulsant, antihyperalgesic, cause sedation and impair motor function. Receptor antagonism may cause convulsions.
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
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Binding
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Human recombinant GABAB(1b) receptors expressed in CHO-K1 cells are used in modified Tris-HCl buffer pH 7.4. A 4 μg‡ aliquot is incubated with 4 nM [³H]CGP-54626 for 180 minutes at 25℃. Non-specific binding is estimated in the presence of 3000 μM GABA. Membranes are filtered and washed, the filters are then counted to determine [³H]CGP-54626 specifically bound. Compounds are screened at 10 μM.
Note: ‡Membrane protein may change from lot to lot, the concentration used will be adjusted if necessary
Ligand:
[³H] CGP-54626
Ligand Kd (nM):
3.6
Ligand Concentration:
4 nM
Non Specific:
3000 µM GABA
Incubation:
180 min at 25°C
Control Inhibitor:
Cgp-54626
Criteria For Significance:
≥ 50% of max stimulation or inhibition
Test Concentration / Dose:
Suggested concentration for initial testing is 10 uM
Test Sample Requirements:
Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).
Minimum Order Quantity:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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