GABAA receptors (GABAARs) mediate neuronal inhibition in the brain. They are the primary targets for benzodiazepines, which are widely used to treat neurological disorders including anxiety, epilepsy and insomnia. The mechanism by which benzodiazepines enhance GABAAR activity has been extensively studied, but there is little mechanistic information on how non-benzodiazepine drugs that bind to t...

GABAergic inputs from at least 18 types of inhibitory interneurons regulate and coordinate the activity of pyramidal cells in the hippocampal area CA1 (Klausberger et al., 2005), which in turn express at least 14 subunits of the GABAA receptor (GABAAR) with varying affinity to GABA and other ligands (Persohn et al., 1992; Wisden et al., 1992; Sperk et al., 1997; Ogurusu et al., 1999). Thus, the...

Inhibitory neurons act in the central nervous system to regulate the dynamics and spatio-temporal co-ordination of neuronal networks. GABA (γ-aminobutyric acid) is the predominant inhibitory neurotransmitter in the brain. It is released from the presynaptic terminals of inhibitory neurons within highly specialized intercellular junctions known as synapses, where it binds to GABAA receptors (GAB...

At concentrations that produce anesthesia, many barbituric acid derivatives act as positive allosteric modulators of inhibitory GABAA receptors (GABAARs) and inhibitors of excitatory nicotinic acetylcholine receptors (nAChRs). Recent research on [H]R-mTFD-MPAB ([H]R-5-allyl-1-methyl-5-(m-trifluoromethyldiazirinylphenyl)barbituric acid), a photoreactive barbiturate that is a potent and stereosel...

Repetitive visual training paired with electrical activation of cholinergic projections to the primary visual cortex (V1) induces long-term enhancement of cortical processing in response to the visual training stimulus. To better determine the receptor subtypes mediating this effect the selective pharmacological blockade of V1 nicotinic (nAChR), M1 and M2 muscarinic (mAChR) or GABAergic A (GABA...