• GABAA a1b2g2

    Concentration dependent activation and desensitization of GABAA (α1β2γ2) receptors by application of 1, 3 and 10 μM GABA as measured on the Port-a-Patch)

GABAA (a1b2g2) - "Patchliner - Investigating the pharmacology of GABAA receptors expressed in HEK293 cells"

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Summary:

γ-amino butyric acid (GABA), β-alanine and bicuculline were investigated on GABAA-receptors expressed in HEK293 cells. The GABAA receptor family is the most important class of inhibitory ion channels involved in synaptic transmission. GABAA receptors are selectively permeable to monovalent anions. They constitute an important therapeutic target for drugs affecting anxiety, sleep and muscle relaxation. In this study, the cells were exposed to compound for 30 s, followed by a 60 s wash step. Solution exchange around the cell was fast, in the order of 50 ms for saturating concentrations. Complete and rapid switching is important when investigating ligand gated ion channels, since the response is often very fast and most receptors desensitize. For rapidly desensitizing ion channels, fast compound application is crucial, so that the entire ion channel population is exposed to maximum concentration before entering the desensitized state. Desensitization and recovery kinetics vary from milliseconds to tens of minutes, depending on receptor type and subunit composition as well as exposure time and/ or compound concentration. Recordings were made in the whole-cell configuration, using the Patchliner (4 amplifier channels). Expected pharmacology was obtained for the investigated compounds.

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