• GABAA a5b3g2

    Pharmacology on GABAA α5β3γ2 as recorded on the SyncroPatch 96, a predecessor model of the SyncroPatch 384PE

GABAA a5b3g2 - "Characterization of hGABAA α5β3γ2 on Nanion's SyncroPatch 96"

icon sp96   SyncroPatch 96 application note, (a predecessor model of the SyncroPatch 384PE)   logo pdf   (0.5 MB)
Cells were kindly provided by Millipore.

Summary:

HEK-cells expressing GABAA-receptors were investigated with the SyncroPatch 96 using a stacked application approach for rapid administration of compounds to the cells. The GABAA receptor family is the most important class of inhibitory ion channels involved in synaptic transmission, and are selectively permeable to monovalent anions. They constitute an important therapeutic area for drugs affecting anxiety, sleep and muscle relaxation. As with most ligand gated ion channels, GABAA exhibit receptor desensitization, which is a common phenomenon for ligand gated ion channels. Desensitization can be either exposure time dependent or concentration dependent, or both. Desensitization and recovery kinetics varies from milliseconds to tens of minutes, all depending on receptor type and subunit composition. For rapidly desensitizing ion channels, it is important that compound application is fast, so that the entire ion channel population is exposed to maximum concentration before entering the desensitized state. Exposure time and application intervals are important factors affecting desensitization and recovery from desensitization, to minimize deletrious effects or receptor desensitization.

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