Human GABA<sub>A</sub> (a<sub>2</sub>β<sub>2</sub>γ<sub>2</sub>) Receptor Cell Line

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  • Concentration-dependent activation of the hGABAA (a2/b2/g2) receptors by the agonist GABA recorded in a membrane potential assay by FLIPRTETRA®. Increasing concentrations of g-aminobutyric acid activated the receptor in a concentration-dependent manner.
  • Channel activation detected as an upward deflection in the fluorescent signal. Recording instrument: FLIPR®.
  • Concentration-response relationship for GABA activation.  The EC50 value was 2.8 µM. Recording instrument: FLIPR®.
  • Reference Compounds (agonist): GABA EC50:  3.2 μM , Isoguvacinel EC50: 1.05 μM
  • Reference Compounds (antagonist): Picrotoxin IC50:  1.9 μM , Ro15-4513 IC50:  61 μM , SR95531 IC50:  0.6 μM

Human GABAA (a2β2γ2) Receptor Cell Line

  • Cat.#:
  • CT6118

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Quick Overview

Human GABAA (α2β2γ2) Receptor-expressing, stable replicating cell line.

Background

The human GABRA2 GABR2 and GABRG2 genes encode the Cl--selective, ionotropic GABAA receptor-channel. GABAA receptors expressed in neurons are therapeutic targets in treatment of neurological and psychological disorders (e.g., seizure and anxiety).
General Info
Product Description Human GABAA (α2β2γ2) Receptor-expressing, stable replicating cell line.
Target Type Ion Channel
Product Type Replicating Cell Line
Family Ligand-Gated
Sub-Type GABAA (a2β2γ2)
Class Ligand-gated cation channel
Therapeutic Area psychiatric disorder, seizure-convulsion
Related Services Large-scale Cryopreservation
Gene Name GABRA2/GABRB2/GABRG2
Validated Assay/Platform FLIPR®
References Olsen, RW and Sieghart W. 2008. Pharmacol Rev. 60:243-260. International Union of Pharmacology. LXX. Subtypes of g-aminobutyric acidA receptors: Classification on the basis of subunit composition.
Liu et al. 2008. Assay and Drug Dev. Tech. 6: 781-786
Host cell CHO-K1
Mycoplasma Status Negative (MycoAlert Kit)
Storage & Packaging
Packaging Cryopreserved cells, 1-2x106 cells
Storage Recommendation liquid nitrogen
Quantity 1-2 million cells
Representative Screening Information
Cell Line CHO-K1 stably expressing human GABA-A (α2β2γ2) receptor
Screening Assay membrane potential dye assay
Readout membrane potential sensitive fluorescent dye
Plate Format 384 well
Instrument FlexStation-III
Signal Window 10.30
Z Score 0.70
DMSO Tolerance <0.5% DMSO
Testing Modes agonist, antagonist, PAM
Testing Options 16-point minimum, 4-point DRC (n = 4), 8-point DRC (n=3 or 4)
Turnaround Time 2 weeks following receipt of Test Articles
Product Documentation
Specification Sheet  Download PDF Document
Screening Info  Download PDF Document