Human GABAA (α<sub>1</sub>/β<sub>2</sub>/γ<sub>2</sub>) Receptor Cell Line

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  • Concentration-dependent inhibition of hGABAA (a1/b2/g2) receptors by picrotoxin recorded by QPatch™. Picrotoxin inhibited the inward currents activated by 30 µM g‑aminobutyric acid.
  • Concentration-response relationship. The IC50 value was 12.8 µM. Recording instrument: QPatch HT™.
  • Reference Compounds (agonist): GABA EC50:  1.3 μM , Isoguvacine EC50: 0.63 μM , CL218872 EC50: 32 μM
  • Reference Compounds (antagonist): Picrotoxin IC50:  9.7 μM , Ro15-4513 IC50:  36 μM , SR95531 IC50:  2.4 μM

Human GABAA (α122) Receptor Cell Line

  • Cat.#:
  • CT6199

Availability: In stock

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Quick Overview

Human GABAA (a1/b2/g2) Receptor-expressing, stable replicating cell line.

Background

The human GABRA1, GABRB2, and GABRG2 genes encode the Cl--selective, ionotropic GABAA receptor-channel. Mutations in GABRA1 have been linked to familial juvenile myoclonic epilepsy. GABAA receptors expressed in CNS neurons are therapeutic targets in treatment seizure and anxiety.
General Info
Product Description Human GABAA (a1/b2/g2) Receptor-expressing, stable replicating cell line.
Target Type Ion Channel
Product Type Replicating Cell Line
Family Ligand-Gated
Sub-Type GABAA122)
Class Ligand-gated channel
Therapeutic Area seizure-convulsion
Related Services Large-scale Cryopreservation
Gene Name GABRA1/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.
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 (α1β2γ2) receptor
Screening Assay membrane potential dye assay
Readout membrane potential sensitive fluorescent dye
Plate Format 384 well
Instrument FlexStation-III
Signal Window 17.99
Z Score 0.80
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