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

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