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...

-Aminobutyric acid type A (GABAA) receptors, a family of Cl -permeable ion channels, mediate fast synaptic inhibition as postsynaptically enriched receptors for -aminobutyric acid at GABAergic synapses. Here we describe an alternative type of inhibitionmediatedbyGABAAreceptors present onneocortical glutamatergic nerve terminals and examine the underlying signaling mechanism(s). By monitoring th...

The effect of GABAA receptor activation varies from inhibition to excitation depending on the state of the transmembrane anionic concentration gradient (delta anion). delta anion was genetically altered in cultured dorsal root ganglion neurons via adenoviral vector-mediated expression of ClC-2, a Cl- channel postulated to regulate the Cl- concentration in neurons in which GABAA receptor activat...

Ionotropic glutamate and gamma-aminobutyric acid type A (GABAA) receptors mediate critical excitatory and inhibitory actions in the brain. Cyclothiazide (CTZ) is well known for its effect of enhancing glutamatergic transmission and is widely used as a blocker for alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)-type glutamate receptor desensitization. Here, we report that in addi...

Background and Purpose ?-Arrestin2 recruitment to ?-receptors may contribute the development of opioid side effects. This possibility led TRV130 PZM21, opioids reportedly biased against ?-arrestin2 in favour G-protein signalling. However, low efficacy by PZM21 simply reflect partial agonism overlooked due overexpression ?-receptors. Experimental Approach Efficacies apparent potencies DAMGO, mor...

GABAA receptors form the major class of inhibitory neurotransmitter receptors in the mammalian brain. This review sets out to summarize the evidence that variations in genes encoding GABAA receptor isoforms are associated with aspects of addictive behaviour in humans, while animal models of addictive behaviour also implicate certain subtypes of GABAA receptor. In addition to outlining the evide...

Presynaptic nerve terminals of inhibitory synapses in the dorsal horn of the spinal cord and brain stem can release both GABA and glycine, leading to coactivation of postsynaptic GABAA and glycine receptors. In the present study we have analyzed functional interactions between GABAA and glycine receptors in acutely dissociated neurons from rat sacral dorsal commissural nucleus. Although the app...

Application of a GABAA (gamma-aminobutyric acid-A) receptor antagonist through a microdialysis probe into the forelimb primary motor cortex of ketamine-anesthetized rats induced electromyographic activity in the contralateral forelimb. This activity consisted of spontaneous forelimb movements with a frequency of 0.8 +/- 0.2 Hz. The motor activity induced by GABAA receptor blockade was suppresse...

Current smoking cessation therapies offer limited success, as relapse rates remain high. Nicotine, which is the major component of tobacco smoke, is thought to be primarily responsible for the addictive properties of tobacco. However, little is known about the molecular mechanisms underlying nicotine relapse, hampering development of more effective therapies. The objective of this study was to ...

GABAA receptors mediate the majority of fast synaptic inhibition in the brain. The accumulation of these ligand-gated ion channels at synaptic sites is a prerequisite for neuronal inhibition, but the molecular mechanisms underlying this phenomenon remain obscure. To further understand these processes, we have examined the cellular origins of synaptic GABAA receptors. To do so, we have created f...