• GABAA a1b3g2

    Pharmacology on GABAA α1β3γ2 as recorded on a multihole (4x) plate (measured on the SyncroPatch 96, a predecessor model of the SyncroPatch 384PE

GABAA Receptor Alpha 1 Beta 3 Gamma 2

GABA Receptors (Cys-loop ligand-gated ion channels)

The GABA receptor family has further been divided into GABAA, GABAB and GABAA-ρ (also called GABAC) receptors.

As typical for Cys-loop receptors, generally four transmembrane spanning domains TM1-TM4 form one receptor subunit, five or four subunits form a pore, several heteromeric combinations are known.
GABAA: Oligomerization of typically five subunits, heteromeric combinations are known of α subunits (GABRA1 - GABRA6), β subunits (GABRB1 - GABRB3) and γ subunits (GABRG1 - GABRG3), as well as δ (GABRD), an ε (GABRE), a π (GABRP), and a θ (GABRQ). The most common type is (α1)2(β2)2(γ2), minimal requirement is  the inclusion of α and β subunits.
GABAB: Heterodimer (GABBR1, GABBR2)
GABAA: Oligomerization of five subunits, heteromeric combinations of three GABAA-ρ subunits are known (GABRR1, GABRR2, GABRR3)

Regulation and Function:
GABAA and GABAA-ρ receptors are ligand-gated ion channels (ionotropic receptors); whereas GABAB receptors are G protein-coupled receptors (metabotropic receptors). All respond to the neurotransmitter gamma-aminobutyric acid (GABA), the main inhibitory transmitter in the mammalian CNS.

Data and Applications

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Application Notes

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GABAA: Further Readings

GABAA receptors - Investigation of Modulators

p37 1 modulatorsicon pl   Patchliner data and applications:
Cells were kindly provided by AstraZeneca.

The top images show dose dependent block of GABAA currents by bicuculline. The IC50 was determined as 1.2 ± 0.2 μM (n=11). The lower graph shows the positive modulation of glycine activation of hGlyRα1. Here, six co-applications of 20 μM glycine and increasing concentrations of a positive modulator are shown.

GABAA Receptor - Stacked Application Technology

p36 3 timedIntervicon pl   Patchliner data and applications:

Ligand gated ion channels often display receptor desensitization. A method was developed to minimize ligand exposure times and intervals between ligand exposures. The pipette first aspirates buffer, then compound. When expelling this stack, the cell is first exposed to ligand and then buffer. Exposure times as low as 400 ms are possible with this method. A GABA dose response curve, aquired in this manner, is shown on the left.

GABAA Receptor - Currents in iCell Neurons

GABA Bicuculline neurons

icon pl   Patchliner data and applications:
Cells were kindly provided by Cellular Dynamics.

Activation of GABAA receptor currents by 30 μM GABA and partial block of the current response by 1 μM bicuculline. Bicuculline was pre-applied for at least 30 s before co-application with GABA (30 μM). Approximately 50% of the current was blocked by 1 μM bicuculline.

2021 - Cell engineering method using fluorogenic oligonucleotide signaling probes and flow cytometry

icon pl  Patchliner publication in Biotechnology Letters (2021)

Shekdar K., Langer J., Venkatachalan S., Schmid L., Anobile J., Shah P., Lancaster A., Babich O., Dedova O., Sawchuck D.

2020 - Novel Expression of GABAA Receptors on Resistance Arteries That Modulate Myogenic Tone

icon sp96   SyncroPatch 96 (a predecessor model of the SyncroPatch 384i) Publication in Journal of Vascular Research (2020)

Yim P.D., Gallos G., Lee-Kong S.A., Dan W., Wu A.D., Xu D., Berkowitz D.E., Emala C.W.

2016 - Automated Patch Clamp Meets High-Throughput Screening: 384 Cells Recorded in Parallel on a Planar Patch Clamp Module

icon sp96  SyncroPatch 384PE (a predecessor model of SyncroPatch 384i) publication in Journal of Lab Automation (2016)

Obergrussberger A., Brüggemann A., Goetze T.A., Rapedius M., Haarmann C., Rinke I., Becker N., Oka T., Ohtsuki A., Stengel T., Vogel M., Steindl J., Mueller M., Stiehler J., George M., Fertig N.

2015 - Novel screening techniques for ion channel targeting drugs

icon pl  Patchliner,   icon sp96   SyncroPatch 384PE (a predecessor model of SyncroPatch 384i) and   Icon CE   CardioExcyte 96 publication in Channels (2015)

Obergrussberger A., Stölzle-Feix S., Becker N., Brüggemann A., Fertig N., Möller C.

2014 - Crystal structure of a human GABAA receptor

icon pap  Port-a-Patch publication in Nature (2014)

Miller P.S., Aricescu A.R.

2012 - Characterizing Human Ion Channels in Induced Pluripotent Stem Cell-Derived Neurons

icon pl   Patchliner publication in Journal of Biomolecular Screening (2012)

Haythornthwaite A, Stoelzle S, Hasler A, Kiss A, Mosbacher J, George M, Brüggemann A, Fertig N.

2009 - Port-a-Patch and Patchliner: High fidelity electrophysiology for secondary screening and safety pharmacology

icon pap  Port-a-Patch and   icon pl   Patchliner publication in Combinatorial Chemistry & High Throughput Screening (2009)

Farre C., Haythornthwaite A., Haarmann C., Stoelzle S., Kreir M., George M., Brüggemann A., Fertig N.

2007 - Automated ion channel screening: patch clamping made easy

icon pap  Port-a-Patch and   icon pl   Patchliner publication in Expert Opinion Therapeutic Targets (2007)

Farre C., Stoelzle S., Haarman C., George M., Brueggemann A., Fertig N.

2006 - Microchip technology for automated and parallel patch clamp recording

icon pap  Port-a-Patch and   icon pl   Patchliner publication in Small Journal (2006)

Brüggemann A., Stoelzle S., George M., Behrends J.C., Fertig N.

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