Robust photoregulation of GABA(A) receptors by allosteric modulation with a propofol analogue. [PDF]
Photochemical switches represent a powerful method for improving pharmacological therapies and controlling cellular physiology. Here we report the photoregulation of GABA(A) receptors (GABA(A)Rs) by a derivative of propofol (2,6-diisopropylphenol), a ...
Bruzik, Karol S +8 more
core +2 more sources
Gephyrin, the enigmatic organizer at GABAergic synapses
GABAA receptors are clustered at synaptic sites to achieve a high density of postsynaptic receptors opposite the input axonal terminals. This allows an efficient propagation of GABA mediated signals, which mostly result in neuronal inhibition.
Verena Eva Tretter +5 more
doaj +1 more source
Differential Modulation of GABAA Receptors Underlies Postsynaptic Depolarization- and Purinoceptor-Mediated Enhancement of Cerebellar Inhibitory Transmission: A Non-Stationary Fluctuation Analysis Study. [PDF]
Cerebellar GABAergic inhibitory transmission between interneurons and Purkinje cells (PCs) undergoes a long-lasting enhancement following different stimulations, such as brief depolarization or activation of purinergic receptors of postsynaptic PCs.
Yumie Ono +2 more
doaj +1 more source
Pathophysiological role of extrasynaptic GABAA receptors in typical absence epilepsy [PDF]
GABA is the principal inhibitory neurotransmitter in the mammalian CNS. It acts via two classes of receptors, the GABAA, a ligand gated ion channel (ionotropic receptor) and the metabotropic G-protein coupled GABAB receptor.
Crunelli, Vincenzo +2 more
core
Pharmacological characterisation of murine α4β1δ GABAA receptors expressed in Xenopus oocytes [PDF]
BACKGROUND: GABAA receptor subunit composition has a profound effect on the receptor's physiological and pharmacological properties. The receptor β subunit is widely recognised for its importance in receptor assembly, trafficking and post-translational ...
Smart, TG, Villumsen, IS, Wellendorph, P
core +1 more source
Ectodermal tissue excised from Xenopus embryos self‐organizes into a three‐dimensional mucociliary organoid. Here, we generate a neural variant, termed neurobot, by implanting neural precursor cells. Neurobots develop mature neurons, adopt distinct morphologies, exhibit more complex motility, and respond differentially to neuroactive compounds. Imaging
Haleh Fotowat +6 more
wiley +1 more source
MUSCARINIC LONG-TERM ENHANCEMENT OF TONIC AND PHASIC GABAA INHIBITION IN RAT CA1 PYRAMIDAL NEURONS
Acetylcholine (ACh) regulates network operation in the hippocampus by controlling excitation and inhibition in rat CA1 pyramidal neurons (PCs), the latter through gamma-aminobutyric acid type-A receptors (GABAARs).
Soledad Dominguez +2 more
doaj +1 more source
The desensitization pathway of GABAA receptors, one subunit at a time
GABAA receptors mediate most inhibitory synaptic transmission in the brain. Here authors used concatemeric α1β2γ2 GABAA receptors to introduce gain-of-desensitization mutations one subunit at a time, revealing non-concerted rearrangements with a key ...
Marc Gielen +2 more
doaj +1 more source
Functional properties of GABAA receptors of AII amacrine cells of the rat retina
Amacrine cells are a highly diverse group of inhibitory retinal interneurons that sculpt the responses of bipolar cells, ganglion cells, and other amacrine cells.
Pablo Beltrán-Matas +2 more
doaj +1 more source
Bottom-Up versus Top-Down Induction of Sleep by Zolpidem Acting on Histaminergic and Neocortex Neurons [PDF]
Zolpidem, a GABAA receptor-positive modulator, is the gold-standard drug for treating insomnia. Zolpidem prolongs IPSCs to decrease sleep latency and increase sleep time, effects that depend on α2 and/or α3 subunit-containing receptors.
Brickley, SG +9 more
core +4 more sources

