Ready-to-Assay™ GABAB Receptor Frozen Cells

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 GABAB-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant GABAB expression on the cell surface and contains high levels of the promiscuous G protein Gα15 to couple the receptor to the calcium signaling pathway. Thus, the cell line is an ideal tool for screening for agonists, antagonists and modulators at GABAB.

Catalog No. Size Price Quantity
HTS119RTA 2 Vials $778.00

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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 (1 ml/vial) of mycoplasma-free cells for one 96-well plate. Includes cell plating media (50 mL).
Storage
Cell vials are to be stored in the vapor phase of liquid N2. Media Component at 4ºC (or -20ºC for prolonged storage).