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MmTX1 and MmTX2 from coral snake venom potently modulate GABAA receptor activity
(2015-02-24)
GABAA receptors shape synaptic transmission by modulating Cl− conductance across the cell membrane. Remarkably, animal toxins that specifically target GABAA receptors have not been identified. Here, we report the discovery ...
MmTX1 and MmTX2 from coral snake venom potently modulate GABAA receptor activity
(2015-02-24)
GABAA receptors shape synaptic transmission by modulating Cl− conductance across the cell membrane. Remarkably, animal toxins that specifically target GABAA receptors have not been identified. Here, we report the discovery ...
Flunitrazepam–Membrane Binding: A Sensor for Drug-Induced GABAA-R and Membrane Structure Changes
(Elsevier Academic Press Inc., 2016)
Flunitrazepam (FNZ) is a sedative–hypnotic benzodiazepine with important therapeutic usefulness and significant abuse liability. Its capability to induce anterograde amnesia favors FNZ use as a “date-rape drug” administered ...
Coupling between GABAA-R ligand-binding activity and membrane organization in β-cyclodextrin-treated synaptosomal membranes from bovine brain cortex: new insights from EPR experiments
(Humana Press, 2012-02)
Correlations between GABAA-receptor (GABAA-R) activity and molecular organization of synaptosomal membranes (SM) were studied along the protocol for cholesterol (Cho) extraction with b-cyclodextrin (b-CD). The mere ...
Acute stress or systemic insulin injection increases flunitrazepam sensitive-GABAA receptor density in synaptosomes of chick forebrain: Modulation by systemic epinephrine
(Taylor & Francis Ltd, 2009-06-07)
Interactions between acute stress and systemic insulin and epinephrine on GABAA receptor density in the forebrain were studied. Here, 10 day-old chicks were intraperitoneally injected with insulin, epinephrine or vehicle ...
Inhibitory effects of carvone isomers on the GABAA receptor in primary cultures of rat cortical neurons
(Wiley, 2014-02)
Carvone is a natural terpene which can be purified as R-(-) or S-(+) enantiomers. There are many reports about its antibacterial, antifungal, and insecticide activities, and also of some effects on the nervous system, where ...
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 ...