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GABAA receptor pharmacology

Pharmacology & Therapeutics, 1995
gamma-Aminobutyric acid (GABA)A receptors for the inhibitory neurotransmitter GABA are likely to be found on most, if not all, neurons in the brain and spinal cord. They appear to be the most complicated of the superfamily of ligand-gated ion channels in terms of the large number of receptor subtypes and also the variety of ligands that interact with ...
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Inhibitory Neurosteroids and the GABAA Receptor

2015
γ-Aminobutyric acid type A receptors (GABAARs) are vital proteins that are engaged in regulating neural circuit activity in the central nervous system. Their effectiveness in this task is dependent on the extent of receptor modulation by naturally occurring ligands that are released in the brain.
Sandra Seljeset   +2 more
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GABAA-receptor subtypes

Trends in Neurosciences, 1996
In a recent issue, a review addressed the important question of which GABAA-receptor subtypes occur in our brain1xMcKernan, R.M. and Whiting, P.J. Trends Neurosci. 1996; 19: 139–143Abstract | Full Text PDF | PubMed | Scopus (939)See all References1.
Kai Kannenberg, Erwin Sigel
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Cyclothiazide binding to the GABAA receptor

Neuroscience Letters, 2008
In order to explore the molecular interaction between cyclothiazide (CTZ) and gamma-aminobutyric acidA (GABAA) receptors, possibly underlying inhibition of GABAA receptor currents, [3H]-CTZ was synthesized. Binding of [3H]-CTZ to rat brain synaptic membranes could be observed only in the presence of the GABAA receptor antagonist (-)[1S,9R]-bicuculline ...
Zoltán Banka   +8 more
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The benzodiazepine binding site of GABAA receptors [PDF]

open access: possibleTrends in Pharmacological Sciences, 1997
The GABAA receptor belongs, along with the nicotinic acetylcholine receptor, the glycine receptor and the 5-HT3 receptor, to a family of homologous transmitter-gated ion channels mediating fast synaptic transmission. Many classes of drug interact with the GABAA receptor, which is the major inhibitory ion channel in the mammalian brain.
Erwin Sigel, Andreas Buhr
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Role of GABAA receptors in cognition

Biochemical Society Transactions, 2009
Complex brains have developed specialized mechanisms for the grouping of principal cells into temporal coalitions of local or distant networks: the inhibitory interneuron ‘clocking’ networks. They consist of GABAergic (where GABA is γ-aminobutyric acid) interneurons of a rich diversity.
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Barbiturates and the GABAA receptor complex

1990
The GABA synapse plays an important role in the pharmacologic effects of barbiturates and the mechanisms involved in barbiturate tolerance and dependence. A synopsis of the effects which have been reported to date is found in Tables 1 and 2. Although the acute changes in neurotransmitter uptake and release are nonselective, a lag in the ability of the ...
Ing K. Ho, Paul A. Saunders
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Surface Expression of GABAA Receptors

Journal of Oral Biosciences, 2010
Abstract The transmission of sensory information to the central nervous system during oral functions such as mastication and swallowing is well regulated by neural networks, including γ-aminobutyric acid (GABA)-mediated inhibitory interneurons. Therefore, an understanding of the mechanism of GABAergic transmission might provide new insight into the ...
Hiroto Tanaka   +5 more
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Multiplicity of GABAA-benzodiazepine receptors

Trends in Pharmacological Sciences, 1989
Binding studies suggest the presence of at least two pharmacologically distinct 'central' benzodiazepine receptors in the brain. Since central benzodiazepine receptors are allosteric modulatory sites on GABAA receptors, this evidence indirectly points to the existence of at least two GABAA receptors.
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Neurosteroids and GABAA receptor function

Trends in Pharmacological Sciences, 1995
In 1984, a potent and selective interaction of the steroidal anaesthetic alphaxalone with the GABAA receptor was demonstrated. Subsequent studies established that certain naturally occurring steroids were potent positive allosteric modulators of the GABAA receptor.
Lambert, Jeremy J.   +3 more
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