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Probes for the heterogeneity of muscimol binding sites in rat brain.
Front Pharmacol
March 2024
Department of Pathobiology of the Nervous System, Center for Brain Research, Medical University of Vienna, Vienna, Austria.
The plant-based alkaloid muscimol is a potent agonist of inhibitory GABA-neurotransmitter receptors. GABA receptors are a heterogeneous family of pentameric complexes, with 5 out of 19 subunits assembling around the central anion pore. Muscimol is considered to bind to all receptor subtypes at the orthosteric drug binding site at the β+/α- interface.
View Article and Find Full Text PDFIncreased GABAA receptor binding in amygdala after prenatal administration of valproic acid to rats.
Acta Neuropsychiatr
October 2017
2Department of Nuclear Medicine and PET Centre, Aarhus University and Hospital,Aarhus,Denmark.
Objective: Prenatal exposure to valproic acid (VPA) enhances the risk for later development of autism spectrum disorders (ASD). An altered gamma-aminobutyric acid (GABA) system may be a key factor in ASD. Here we investigated possible changes in the GABA system in rats exposed to a low dose of prenatal VPA.
View Article and Find Full Text PDFPrevention of an increase in cortical ligand binding to AMPA receptors may represent a novel mechanism of endogenous brain protection by G-CSF after ischemic stroke.
Restor Neurol Neurosci
August 2016
Institute of Neuropathology, University Medical Center of the Johannes Gutenberg University, Mainz, Germany.
Purpose: Using G-CSF deficient mice we recently demonstrated neuroprotective properties of endogenous G-CSF after ischemic stroke. The present follow-up study was designed to check, whether specific alterations in ligand binding densities of excitatory glutamate or inhibitory GABAA receptors may participate in this effect.
Methods: Three groups of female mice were subjected to 45 minutes of MCAO: wildtype, G-CSF deficient and G-CSF deficient mice substituted with G-CSF.
Background: GABA(A) receptors (GABA(A)R) are composed of several subunits that determine sensitivity to drugs, synaptic localisation and function. Recent studies suggest that agonists targeting selective GABA(A)R subunits may have therapeutic value against the cognitive impairments observed in schizophrenia. In this study, we determined whether GABA(A)R binding deficits exist in the dorsolateral prefrontal cortex (DLPFC) of people with schizophrenia and tested if changes in GABA(A)R binding are related to the changes in subunit mRNAs.
View Article and Find Full Text PDFIn vitro neuropharmacological evaluation of penitrem-induced tremorgenic syndromes: importance of the GABAergic system.
Neurochem Int
December 2011
Section of Chemistry and Toxicology, Norwegian Veterinary Institute, P.O. Box 750, Sentrum, N-0106 Oslo, Norway.
The effects of the fungal neurotoxin penitrem A on the GABAergic and glutamatergic systems in rat brain were evaluated. Penitrem A inhibited binding of the GABA(A)-receptor ligand [³H]TBOB to rat forebrain and cerebellar membrane preparations with IC₅₀ (half maximal inhibitory concentration) values of 11 and 9 μM, respectively. Furthermore, penitrem A caused a concentration-dependent increase of [³H]flunitrazepam and [³H]muscimol binding in rat forebrain, but not in cerebellar preparations.
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