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The Mechanism of Enantioselective Neurosteroid Actions on GABAA Receptors
The neurosteroid allopregnanolone (ALLO) and pregnanolone (PREG), are equally effective positive allosteric modulators (PAMs) of GABAA receptors. Interestingly, the PAM effects of ALLO are strongly enantioselective, whereas those of PREG are not.
Hiroki Tateiwa+10 more
doaj +1 more source
New GABA amides activating GABAA-receptors [PDF]
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
Raster, Peter+5 more
openaire +5 more sources
Background γ-aminobutyric acid (GABA) is an important inhibitory neurotransmitter which mainly mediates its effects on neurons via ionotropic (GABAA) and metabotropic (GABAB) receptors.
Bettler Bernhard+6 more
doaj +1 more source
Allosteric modulation of retinal GABA receptors by ascorbic acid [PDF]
Ionotropic GABA receptors (GABAA and GABAC) belong to the Cys-loop receptor family of ligand-gated ion channels. GABAC receptors are highly expressed in the retina, mainly localized at the axon terminals of bipolar cells.
Aguayo, Luis G.+5 more
core +1 more source
Anaesthetic impairment of immune function is mediated via GABA(A) receptors.
BackgroundGABA(A) receptors are members of the Cys-loop family of neurotransmitter receptors, proteins which are responsible for fast synaptic transmission, and are the site of action of wide range of drugs.
Daniel W Wheeler+15 more
doaj +1 more source
Insights into GABA receptor signalling in TM3 Leydig cells [PDF]
gamma-Aminobutyric acid (GABA) is an emerging signalling molecule in endocrine organs, since it is produced by endocrine cells and acts via GABA(A) receptors in a paracrine/autocrine fashion.
Artur Mayerhofer+28 more
core +2 more sources
Investigating the Role of Loop C Hydrophilic Residue 'T244' in the Binding Site of ρ1 GABAC Receptors via Site Mutation and Partial Agonism. [PDF]
The loop C hydrophilic residue, threonine 244 lines the orthosteric binding site of ρ1 GABAC receptors was studied by point mutation into serine, alanine and cysteine, and tested with GABA, some representative partial agonists and antagonists. Thr244 has
Moawiah M Naffaa+5 more
doaj +1 more source
Stress and GABAAreceptors [PDF]
J. Neurochem.(2010)112, 1115–1130.AbstractGABAAreceptors are sensitive to subtle changes in the environment in both early‐life and adulthood. These neurochemical responses to stress in adulthood are sex‐dependent. Acute stress induces rapid changes in GABAAreceptors in experimental animals, with the direction of the changes varying according to the sex
Kelly J. Skilbeck+2 more
openaire +3 more sources
Filial imprinting of domestic chicks has a well-defined sensitive (critical) period lasting in the laboratory from hatching to day 3. It is a typical model to investigate the molecular mechanisms underlying memory formation in early learning. We recently
Naoya Aoki+7 more
doaj +1 more source
Multiple and plastic receptors mediate tonic GABAA receptor currents in the hippocampus [PDF]
Persistent activation of GABAA receptors by extracellular GABA (tonic inhibition) plays a critical role in signal processing and network excitability in the brain.
Kullmann, D.M.+4 more
core +1 more source