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

PubChem ID

119

Name

4-aminobutyric acid

Measurement

>10μM - IC50

PubChem ID

3380

Name

Flunitrazepam

Measurement

>10μM - IC50

PubChem ID

197584

Name

Cgp-54626

Measurement

0.0063μM - IC50

PubChem ID

Name

Picrotoxin

Measurement

>10μM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

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