ChemiScreen™ GABAB Receptor Stable Cell Line

The neurotransmitter g-aminobutyric acid (GABA) exerts its effects through an ion channel, GABAA, and a GPCR, GABAB. Functional GABAB is a heterodimer composed of the GABAB1 and GABAB2 subunits, which share 35% sequence identity and belong to the class 3 family of GPCRs. The GABAB1 subunit, which exists as splice variants GABAB1a and GABAB1b, binds directly to GABA and is required for agonist activation. The GABAB2 and GABAB1 subunits associate by formation of a coiled coil by their C-terminal tails; this association masks an ER retention sequence in GABAB1 to permit export from the ER and trafficking to the cell surface. In addition to its chaperone function, GABAB2 is the component that couples to Gi to reduce intracellular cAMP. Agonists of GABAB, such as baclofen, are used clinically for treatment of muscle spasticity, migraine headache and musculoskeletal pain (Bowery et al., 2002). Cloned human GABAB1b/GABAB2 receptor-expressing ChemiScreen cells were constructed by stable transfection of Chem-1 cells with GABAB1b/GABAB2 which supports high levels of recombinant GABAB1b/GABAB2 expression on the cell surface and contains high levels of the promiscuous G protein Gα15 to couple the receptor to the calcium signaling pathway. These stability-tested cells are ready for fluorescence-based assays for agonists, antagonists and modulators at the GABAB receptor.

Catalog No. Size Price Quantity
HTS119C 2 Vials $18,779.00

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Application
Calcium Flux Assay
Family
GABAB
Target
GABAB
Accession Number
NM_021903, NM_005458
Species
Human
Host Cell Type
Chem-1
Content
2 Vials of mycoplasma-free cells, 1 ml per vial
Storage
Cell vials are to be stored in the vapor phase of liquid N2.
  • [User Manual] ChemiSCREEN™ and ChemiBRITE™ Cell Lines

    The ChemiSCREEN and ChemiBRITE Cell Lines are designed to enable the measurement of intracellular calcium levels when a GPCR of interest has been activated by a ligand. These cell lines are suitable for studying small molecules as well as biologics. The assay protocol has been optimized for use in either a 384-well or 96-well format.

    ChemiSCREEN and ChemiBRITE cells stably expres...

    [User Manual] ChemiSCREEN™ and ChemiBRITE™ Cell Lines