The mAb 62-3G1 to the GABAA receptor/benzodiazepine receptor/Cl- channel complex was used with light-microscopy immunocytochemistry for studying the localization of the GABAA receptors (GABAR) in the rat brain. The results have shown a receptor distribution identical to the one obtained by others using 3H-muscimol binding in combination with autoradiographic techniques. The external plexiform l...

The neurotransmitter gamma-aminobutyric acid (GABA) inhibits the activity of signal-receiving neurons by interacting with the GABAA receptor on these cells. The GABAA receptor is a channel-forming protein that allows the passage of chloride ions into the cells. Excessive GABAA activation may play a role in mediating the sedative effects of alcohol and other sedating and anesthetic agents. For e...

The inhibitory glycine receptor (nomenclature as agreed by the NC-IUPHAR Subcommittee on Glycine Receptors) is a member of Cys-loop superfamily transmitter-gated ion channels that includes zinc activated channels, GABAA, nicotinic acetylcholine and 5-HT3 receptors Zn2+- channels. expressed either homo-pentamer α subunits, or complex now thought to harbour 2α 3β subunits [33, 7], contain an intr...

The whisker-to-barrel system of adult mice was used in a study on the effects of short-lasting tactile stimulation and sensory conditioning training on GABAA receptor binding in the barrel field of somatosensory cortex. In vitro receptor binding autoradiography was used to examine the pattern and intensity of [3H]muscimol binding to GABAA receptors. A well-defined pattern of GABAA receptors in ...

αβγ GABAA receptor currents are phasic and desensitizing while αβδ GABAA receptor currents are tonic and have no fast desensitization. αβγ receptors are subsynaptic and mediate phasic inhibition while αβδ receptors are extra or peri-synaptic and mediate tonic inhibition. Given the different roles of these GABAA receptor isoforms and that GABAA receptors are allosterically regulated by extracell...

We have prepared a series of new and some literature-reported GABA-amides and determined their effect on the activation of GABAA-receptors expressed in CHO cells. Special attention was paid to the purification of the target compounds to remove even traces of GABA contaminations, which may arise from deprotection steps in the synthesis. GABA-amides were previously reported to be partial, full or...

A successful unified pharmacophore/receptor model which has guided the synthesis of subtype selective compounds is reviewed in light of recent developments both in ligand synthesis and structural studies of the binding site itself. The evaluation of experimental data in combination with a comparative model of the 1 2 2 GABAA receptor leads to an orientation of the pharmacophore model within the...

In the CNS, gamma-aminobutyric acid (GABA) affects neuronal activity through both the ligand-gated GABAA receptor channel and the G protein-coupled GABAB receptor. In the mature nervous system, both receptor subtypes decrease neural excitability, whereas in most neurons during development, the GABAA receptor increases neural excitability and raises cytosolic Ca2+ levels. We used Ca2+ digital im...