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GABA-induced uncoupling of GABA/benzodiazepine site interactions is mediated by increased GABAA receptor internalization and associated with a change in subunit composition
(Elsevier, 2014-01)
Persistent activation of GABAA receptors triggers compensatory changes in receptor function that are relevant to physiological, pathological and pharmacological conditions. Chronic treatment of cultured neurons with GABA ...
Flavonoids as GABAA receptor ligands: the whole story?
(Dove Medical Press, 2012-01)
Benzodiazepines are the most widely prescribed class of psychoactive drugs in current therapeutic use, despite the important unwanted side effects that they produce, such as sedation, myorelaxation, ataxia, amnesia, and ...
GABA induces activity dependent delayed-onset uncoupling of GABA/benzodiazepine site interactions in neocortical neurons
(American Society for Biochemistry and Molecular Biology, 2005-06)
Changes in the function of type A γ-aminobutyric acid receptors (GABAARs) are associated with neuronal development and tolerance to the sedative-hypnotic effects of GABAAR positive modulators. Persistent activation of ...
6-Chloro-3'-nitroflavone is a potent ligand for the benzodiazepine binding site of the GABA(A) receptor devoid of intrinsic activity
(Pergamon-Elsevier Science Ltd, 2000-12)
6-Chloro-3'-nitroflavone integrates a list of nearly 70 flavone derivatives synthesized in our laboratories. The effects of 6-chloro-3'- nitroflavone on the benzodiazepine binding sites (BDZ-BSs) of the GABA(A) receptor ...
Orthosteric and benzodiazepine cavities of the α1β2γ2 GABAA receptor: insights from experimentally validated in silico methods
(Adenine Press, 2019-05-04)
γ-aminobutyric acid-type A (GABA A ) receptors mediate fast synaptic inhibition in the central nervous system of mammals. They are modulated via several sites by numerous compounds, which include GABA, benzodiazepines, ...
QSAR modeling of the interaction of flavonoids with GABA(A) receptor
(Elsevier France-editions Scientifiques Medicales Elsevier, 2008-08)
Experimentally assigned values to binding affinity constants of flavonoid ligands towards the benzodiazepine site of the GABA(A) receptor complex were compiled from several publications, and enabled to perform a predictive ...
The neuronal GABAA receptor as target for therapeutic and toxic chemical compounds: In vitro studies using cultured cortical neurons
(Asociación de Químicos e Ingenieros, 2007-12)
Los neurotransmisores son sustancias químicas liberadas por las neuronas y reconocidas por proteínas o receptores específicos situados en la membrana celular. El control de la neurotransmisión excitadora e inhibidora es ...
Valepotriate Hydrines Isolated from an Anticonvulsant Fraction of Valeriana pavonii Poepp. & Endl
(Colegio Farmaceuticos Provincia de Buenos Aires, 2013-08)
The present study deals with the isolation and identification of three valepotriate hydrines that are first reported in Valeriana pavonii Poepp. & Endl. (Valerianaceae), which were obtained from a dichloromethane fraction ...
(±)-1-(2,5-dimethoxy-4-ethylthiophenyl)-2-aminopropane (ALEPH-2), a novel putative anxiolytic agent lacking affinity for benzodiazepine sites and serotonin-1A receptors
(Springer Verlag, 1996)
Serotonergic behavioral responses, effects on motor activity and core temperature, and binding properties of the novel putative anxiolytic amphetamine derivative (±)1-(2,5-dimethoxy-4-ethylthiophenyl)-2-aminopropane ...