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Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABAA receptor α1 subtype
TLDR
This work created genetically modified mice with a diazepam-insensitive α1 subtype and a selective BZ site ligand to explore GABAA receptor subtypes mediating specific physiological effects and revealed that the α1Subtype mediated the sedative, but not the anxiolytic effects of benzodiazepines. Expand
Which GABAA-receptor subtypes really occur in the brain?
TLDR
It is concluded that the number of major subtypes is probably less than ten but their physiological roles have yet to be clearly defined and this represents the next step in GABAA-receptor research. Expand
Enhanced Learning and Memory and Altered GABAergic Synaptic Transmission in Mice Lacking the α5 Subunit of the GABAAReceptor
TLDR
Data suggest that α5-containing GABAA receptors play a key role in cognitive processes by controlling a component of synaptic transmission in the CA1 region of the hippocampus. Expand
Evidence for a Significant Role of α3-Containing GABAA Receptors in Mediating the Anxiolytic Effects of Benzodiazepines
TLDR
Data show that potentiation of α3-containing GABAA receptors is sufficient to produce the anxiolytic effects of BZs and that α2 potentiation may not be necessary. Expand
[3H]L-655,708, a Novel Ligand Selective for the Benzodiazepine Site of GABAA Receptors which Contain the α5 Subunit
TLDR
It is concluded that [3H]L-655,708 is the first radioligand to date which is selective for any BZ2 subtype of the GABAA receptor and should provide a valuable tool for elucidating the structure and function of the alpha 5-containing GabAA receptor subtype. Expand
L-655,708 enhances cognition in rats but is not proconvulsant at a dose selective for α5-containing GABAA receptors
TLDR
In the Morris water maze, L-655,708 enhanced performance not only during acquisition but also in a probe trial, demonstrating that this compound has cognition enhancing effects, and further support the potential of alpha5-containing GABA(A) receptors as a target for novel cognition enhancing drugs. Expand
NMDA receptor pathways as drug targets
TLDR
The future prospects for drugs that act on NMDA receptor pathways are critically assessed, including potential treatments for some major disorders such as stroke and Alzheimer's disease, for which effective therapies are still lacking. Expand
Sedation and Anesthesia Mediated by Distinct GABAA Receptor Isoforms
TLDR
Findings show that anesthesia and sedation are mediated by distinct GABAA receptor subtypes, and that the β2 subunit mediates the sedative properties of anesthetics. Expand
Loss of the Major GABAA Receptor Subtype in the Brain Is Not Lethal in Mice
TLDR
It is confirmed that α1β2γ2 is the major GABAA receptor subtype in the murine brain and it is demonstrated that, surprisingly, the loss of this receptor sub type is not lethal. Expand
Pharmacological reversal of a pain phenotype in iPSC-derived sensory neurons and patients with inherited erythromelalgia
TLDR
A selective Nav1.7 sodium channel blocker reduced hyperexcitability of iPSC-derived sensory neurons and alleviated pain in a subpopulation of patients with an inherited pain disorder, providing proof of principle that selective Nav 1.7 blockade may be useful in pain alleviation. Expand
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