Results 21 to 30 of about 84,762 (274)
Archiv der Pharmazie, Volume 356, Issue 1, January 2023., 2023 Combining ligand‐based and structure‐based methodologies, the applied virtual screening approach identified a collection of sulfonamides targeting the human carbonic anhydrase (hCA) VA isoform. 2‐(3,4‐Dihydro‐2H‐quinolin‐1‐yl)‐N‐(4‐sulfamoylphenyl)acetamide was identified as a potent and selective lead compound as a candidate for further exploitation ...
Laura De Luca +4 more
wiley +1 more source
Direct imaging of lateral movements of AMPA receptors inside synapses [PDF]
EMBO J 22, 18 (15/09/2003) 4656-65, 2007 Trafficking of AMPA receptors in and out of synapses is crucial for synaptic plasticity. Previous studies have focused on the role of endo/exocytosis processes or that of lateral diffusion of extra-synaptic receptors. We have now directly imaged AMPAR movements inside and outside synapses of live neurons using single-molecule fluorescence microscopy ...
arxiv +1 more source
New GABA amides activating GABAA-receptors [PDF]
Beilstein Journal of Organic Chemistry, 2013 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
Brazilian Journal of Medical and Biological Research, 2001 The aim of the present study was to determine if phenobarbital affects the nociception threshold. Systemic (1-20 mg/kg) phenobarbital administration dose dependently induced hyperalgesia in the tail-flick, hot-plate and formalin tests in rats and in the ...
C.M. Yokoro +4 more
doaj +1 more source
The Mechanism of Enantioselective Neurosteroid Actions on GABAA Receptors
Biomolecules, 2023 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
Brain and Behavior, Volume 12, Issue 12, December 2022., 2022 Considering the complications related to alcohol withdrawal syndrome (AWS) such as seizure, delirium tremens and cardiac arrhythmia, it is important to identify the risk of delirium tremens (DT) following AWS and enhance preventive strategies. We observed the characteristics of quantitative electroencephalography in patients with AWS, specifically who ...
Jee‐Eun Yoon +3 more
wiley +1 more source
Molecular Pain, 2009 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
Large number of receptors may reduce cellular response time variation [PDF]
Physical biology 10 (3), 035008, 2013, 2012 Cells often have tens of thousands of receptors, even though only a few activated receptors can trigger full cellular responses. Reasons for the overabundance of receptors remain unclear. We suggest that, in certain conditions, the large number of receptors results in a competition among receptors to be the first to activate the cell.
arxiv +1 more source
Investigating the Role of Loop C Hydrophilic Residue 'T244' in the Binding Site of ρ1 GABAC Receptors via Site Mutation and Partial Agonism. [PDF]
PLoS ONE, 2016 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]
Journal of Neurochemistry, 2010 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