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Pharmacological modulation of GABAA receptors

Current Opinion in Pharmacology, 2021
Ligand-gated ion channels are integral membrane proteins that activate through a change in conformation upon transmitter binding and were identified as key players of brain function. GABAA receptors are major inhibitory ligand-gated ion channels of this protein family.
Frédéric Knoflach, Daniel Bertrand
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An update on GABAA receptors

Brain Research Reviews, 1999
Recent advances in molecular biology and complementary information derived from neuropharmacology, biochemistry and behavior have dramatically increased our understanding of various aspects of GABAA receptors. These studies have revealed that the GABAA receptor is derived from various subunits such as alpha1-alpha6, beta1-beta3, gamma1-gamma3, delta ...
Maharaj K. Ticku, Ashok K. Mehta
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Molecular Biology of the GABAA Receptor

1988
The GABAA receptorreceptor is the major molecular site of the ubiquitous inhibitory acEivities of the brain, being present on the great majority of mammalian brain neurones (1). Electrophysiological studies and, especially, recent patch-clamp studies on cultured neurones (2,3) have established that at these sites GABA opens a chloride channel which is ...
Barnard, E.   +9 more
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Neurosteroid modulation of GABAA receptors

Progress in Neurobiology, 2003
Certain metabolites of progesterone and deoxycorticosterone are established as potent and selective positive allosteric modulators of the gamma-aminobutyric acid type A (GABA(A)) receptor. Upon administration these steroids exhibit clear behavioural effects that include anxiolysis, sedation and analgesia, they are anticonvulsant and at high doses ...
Lambert, Jeremy J.   +4 more
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Molecular Neurobiology of the GabaA Receptor

1994
Publisher Summary This chapter discusses the molecular neurobiology of the GABAA receptor. The GABAA receptor is responsible for the majority of neuronal inhibition in the vertebrate CNS. The ubiquitous distribution of the GABAA receptor in the mammalian CNS is revealed by the use of [3H]GABA radioligand binding techniques, whereas autoradiographic ...
Alan N. Bateson   +2 more
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The GABAA Receptors

1996
Transmitter-gated ion channels are multisubunit membrane-spanning receptors that serve as rapid signal transduction devices regulating the flow of cations or anions through the cell membrane. Cell type—specific flexibility in neurotransmission is accomplished by a multiplicity of channel variants based on the combinatorial assembly of structurally ...
Bernhard Lüscher   +5 more
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