Pharmacological evaluation of GABAA receptor subtypes on Qube 384

Ligand-gated experiments require many compound additions for incubation, stimulation, test drug and combinations thereof. Enabling that in 384-format tremendously enhances the throughput which is necessary to find the interesting new NAMs, PAMs or other types of compounds.

Here we report studies of three subtypes of GABAA channels using Qube 384 and with focus on:

• Short ligand exposure with repetitive stimulations with EC50 concentrations of GABA
• Effects of agonists, antagonists and modulators
• Cumulative and non-cumulative concentration-response relationships
• Characterizing the pharmacological properties of four cell lines expressing different GABAA subtypes

For the full application report, please see here.

Two new posters by Charles River Laboratories on HTS ion channel screening

Using the stacked solution technology Charles River have developed and validated an assay suited for high through screening on both P2X- and GABA receptors. The short exposure of ligand of less than 1 second enables repetitive stimulation which is necessary for this assay. In another assay with voltage-gated target, the vast number of parameters that can be measured with high fidelity e-phys makes it important that the underlying software is powerful enough to cope. Read more here for ligand-gated and here for the Na_V1.1 assay.

GABA receptors – HTS electrophysiology and optopharmacology on primary cells and stable cell lines

GABA is an important neurotransmitter in CNS, which controls most of the functions of the body and mind. It’s has been implicated in several health challenges such as anxiety disorders, insomnia, or depression. In this poster, we show pharmacological modulation of GABAAR using QPatch and Qube 384. The study includes a characterization of the heterogeneous GABAAR population of cultured primary hippocampal astrocytes and an evaluation of the GABAAR clone ɑ5β3γ2.

The results demonstrate the feasibility of performing GABAAR-targeted drug-screening on Qube and QPatch, and we also introduce optopharmacology as a viable application possibility for high-throughput pharmacological experiments.

See the poster here.

GABAA pharmacology on cell lines and primary astrocytes on QPatch

In this new Sophion Application report  GABA receptor pharmacology was evaluated on QPatch. We did thorough compound evaluations in a GABAA(α5β3γ2) cell line and investigated the GABA response of primary hippocampal rat astrocytes with emphasis on:

• Effects of agonists, antagonists, and modulators
• Concentration-response relationships
• EC₅₀ and IC₅₀ determination
• Characterizing both the pharmacology of a specific isolated GABAA subtype and the physiological GABA response of cultured rat astrocytes

Read the full report here.

Also, you are welcome to check out our other publications on GABA here.