Human GABA<sub>A</sub> (a<sub>5</sub>β<sub>2</sub>γ<sub>2</sub>) Receptor Cell Line

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  • Concentration-dependent activation of the hGABAA (a5/b2/g2) receptor by the agonist GABA measured with a membrane potential assay in 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.
  • Concentration-response relationship for GABAA activation. The EC50 value was 4.7 µM. Recording instrument: FLIPR®.

Human GABAA (a5β2γ2) Receptor Cell Line

  • Cat.#:
  • CT6119

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Quick Overview

Human GABAA (α5β2γ2) Receptor-expressing, stable replicating cell line.

Background

The human GABRA5 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., cognitive impairment and schizophrenia).
General Info
Product Description Human GABAA (α5β2γ2) Receptor-expressing, stable replicating cell line.
Target Type Ion Channel
Product Type Replicating Cell Line
Family Ligand-Gated
Sub-Type GABAA (a5β2γ2)
Class Ligand-gated cation channel
Therapeutic Area psychiatric disorder, pulmonary-respiratory, seizure-convulsion
Related Services Large-scale Cryopreservation
Gene Name GABRA5/GABRB2/GABRG2
Validated Assay/Platform FLIPR®, QPatch HT
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.
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 (α5β2γ2) receptor
Screening Assay membrane potential dye assay
Readout membrane potential sensitive fluorescent dye
Plate Format 384 well
Instrument FlexStation-III
Signal Window 11.60
Z Score 0.73
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