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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.
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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.
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L-655,708 enhances cognition in rats but is not proconvulsant at a dose selective for α5-containing GABAA receptors
View on Elsevier
Cholinergic correlates of cognitive impairment in Parkinson's disease: comparisons with Alzheimer's disease.
TLDR
In Parkinson's but not Alzheimer's disease the decrease in neocortical (particularly temporal) choline acetyltransferase correlated with the number of neurons in the nucleus of Meynert suggesting that primary degeneration of these cholinergic neurons may be related, directly or indirectly, to declining cognitive function in Parkinson's disease.
View on BMJ
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.
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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.
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TPA023 [7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine], an Agonist Selective for α2- and α3-Containing GABAA Receptors, Is a…
TLDR
The novel α2/α3-selective efficacy profile of TPA023 translates into a nonsedating anxiolytic profile that is distinct from nonselective agonists.
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Molecular Forms of Acetylcholinesterase and Butyrylcholinesterase in the Aged Human Central Nervous System
TLDR
Although the patterns of molecular forms of each enzyme were broadly similar among the different areas, regional variations in the distribution and abundance of the various forms of AChE were much greater than those of BChE, and these findings are discussed in relation to neurochemical and neuroanatomical features of the regions examined.
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Selective Blockade of 5-Hydroxytryptamine (5-HT)7 Receptors Enhances 5-HT Transmission, Antidepressant-Like Behavior, and Rapid Eye Movement Sleep Suppression Induced by Citalopram in Rodents
TLDR
Results indicate that selective blockade of 5-HT7 receptors may enhance the antidepressant efficacy of citalopram and may provide a novel therapy to alleviate sleep disturbances associated with depression.
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The benzodiazepine binding site of GABAA receptors as a target for the development of novel anxiolytics
  • J. Atack
  • Biology, Psychology
    Expert opinion on investigational drugs
  • 1 May 2005
TLDR
The advent of molecular genetic and pharmacological approaches has begun to delineate which GABAA receptor subtypes are associated with the various pharmacological effects of the non-selective BZs, raising the possibility of a compound that selectively modulates α2- and/or α3- containing receptors but does not affect α1-containing receptors would be a non-sedating anxiolytic.
View on Taylor & Francis
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