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Neurosteroids and GABAA receptor function
Trends in Pharmacological Sciences, 1995In 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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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 ...
H. Mohler +5 more
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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 ...
H. Mohler +5 more
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Neurosteroid modulation of GABAA receptors
Progress in Neurobiology, 2003Certain 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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Cyclothiazide binding to the GABAA receptor
Neuroscience Letters, 2008In 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 ...
Eva, Szárics +8 more
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Molecular Neurobiology of the GabaA Receptor
1994Publisher 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 ...
S M, Dunn, A N, Bateson, I L, Martin
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The diversity of GABAA receptors
Molecular Neurobiology, 1998The amino acid gamma-aminobutyric-acid (GABA) prevails in the CNS as an inhibitory neurotransmitter that mediates most of its effects through fast GABA-gated Cl(-)-channels (GABAAR). Molecular biology uncovered the complex subunit architecture of this receptor channel, in which a pentameric assembly derived from five of at least 17 mammalian subunits ...
W, Hevers, H, Lüddens
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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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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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Role of GABAA receptors in cognition
Biochemical Society Transactions, 2009Complex 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
1990The 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 ...
P A, Saunders, I K, Ho
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Inhibitory Neurosteroids and the GABAA Receptor
2015γ-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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