Recording of GABAA receptor-mediated Cl- currents

GABA (Gama-amino buytyric acid) is the primary inhibitory neurotransmitter in the central nervous system. GABAA receptors belong to a family of ligand gated ion channels medi- ating fast synaptic transmission. They are of major importance as pharmacological tar- gets for anxiolytics (e.g. benzodiazepines), schizophrenia, and sleep aids. At least nine- teen different individual GABAA receptor subunits assemble into pentameric structures in different combinations to form the native receptor (α1-6, β1-3, γ1-3, δ, ρ1-3, plus minor subunits)1. When activated, these receptor/channels conduct a Cl-current that desensitizes at higher GABA concentrations, with a characteristic rate for different sub- unit combinations. Receptors containing α1-5 subunits, any β subunits, and the γ2 sub- unit are the most prevalent in the brain. These receptors are sensitive to benzodiazepine modulation. The search for subtype-selective drugs for GABAA channels has been ham- pered by the lack of suitable high throughput electrophysiology platforms with the ability to interrogate ligand gated channels.


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