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N,N′-Dicyclohexylsulfamide and N,N′-diphenethylsulfamide are anticonvulsant sulfamides with affinity for the benzodiazepine binding site of the GABAA receptor and anxiolytic activity in mice
(Elsevier Inc, 2012-01)
A set of sulfamides designed, synthesized and evaluated against maximal electroshock seizure (MES) and pentilenetetrazol (PTZ) tests with promising results, were tested for their affinity for the benzodiazepine binding ...
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 ...
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 ...
Central nervous system activities of two diterpenes isolated from Aloysia virgata
(Elsevier Gmbh, 2011-03)
Using the guide of a competitive assay for the benzodiazepine binding site in the γ-aminobutyric acid type A receptor (GABAA), two active diterpenes were isolated from the aerial parts of Aloysia virgata (Ruíz & Pavón) ...
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 ...
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, ...
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 ...
GABAergic modulation with classical benzodiazepines prevent stress-induced neuro-immune dysregulation and behavioral alterations
(2016)
Objective: Psychosocial stress is associated with altered immunity, anxiety, and depression. Repeated
social defeat (RSD), a model of social stress, triggers egress of inflammatory myeloid progenitor cells
(MPCs; ...
Synthesis and pharmacological evaluation of pyrazolo[4,3-c]quinolinones as high affinity GABAA-R ligands and potential anxiolytics
(Pergamon-Elsevier Science Ltd, 2018-08)
The synthesis, in vitro ligand binding study and in vivo Elevated Plus Maze test (EPM) of a series of pyrazolo[4,3-c]quinolin-3-ones (PQs) are reported. Multistep synthesis of PQs started from anilines and diethyl ...
Synthesis and pharmacological evaluation of pyrazolo[4,3-c]quinolinones as high affinity GABAA-R ligands and potential anxiolytics
(Elsevier, 2018-08-07)
The synthesis, in vitro ligand binding study and in vivo Elevated Plus Maze test (EPM) of a series of pyrazolo[4,3-c]quinolin-3-ones (PQs) are reported. Multistep synthesis of PQs started from anilines and diethyl ...