Chemical Name: 11,12,13,13a-Tetrahydro-7-methoxy-9-oxo-9H-imidazo[1,5-a]pyrrolo[2,1-c][1,4]benzodiazepine-1-carboxylic acid, ethyl ester
Biological ActivityPotent, selective inverse agonist for the benzodiazepine site of GABAA receptors containing the α5 subunit (Ki = 0.45 nM). Displays 50-100-fold selectivity over GABAA receptors containing α1, α2, α3 or α6 subunits in combination with β3 and γ2. Enhances LTP in a mouse hippocampal slice model and increases spatial learning, without displaying proconvulsant activity.
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For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
L-655,708 enhances cognition in rats but is not proconvulsant at a dose selective for α5-containing GABAA receptors.
Atack et al.
[3H]L-655,708, a novel ligand selective for the benzodiazepine site of GABAA receptors which contain the α5 subunit.
Quirk et al.
Rat and human hippocampal α5 subunit-containing γ-aminobutyric acidA receptors have α5α3γ2 pharmacological characteristics.
Sur et al.
Citations for L-655,708
The citations listed below are publications that use Tocris products. Selected citations for L-655,708 include:
8 Citations: Showing 1 - 8
Comparison of rapid and long-lasting antidepressant effects of negative modulators of α5-containing GABAA receptors and (R)-ketamine in a chronic social defeat stress model.
Authors: Xiong Et al.
GABAA Receptor Subtypes Regulate Stress-Induced Colon Inflammation in Mice.
Authors: Seifi Et al.
Diminished KCC2 confounds synapse specificity of LTP during senescence.
Authors: Ferando Et al.
Nat Neurosci 2016;19:1197
Reduction in focal ictal activity following transplantation of MGE interneurons requires expression of the GABAA receptor α4 subunit.
Authors: Jaiswal Et al.
J Neurosci 2015;9:127
Molecular and functional diversity of GABA-A receptors in the enteric nervous system of the mouse colon.
Authors: Seifi Et al.
Stem Cells Dev 2014;34:10361
Enhancing the function of alpha5-subunit-containing GABAA receptors promotes action potential firing of neocortical neurons during up-states.
Authors: Drexler Et al.
Eur J Pharmacol 2013;703:18
Modulation of α5 subunit-containing GABAA receptors alters alcohol drinking by rhesus monkeys.
Authors: Rüedi-Bettschen Et al.
Alcohol Clin Exp Res 2013;37:624
Chronic exposure to anabolic androgenic steroids alters neuronal function in the mammalian forebrain via androgen receptor- and estrogen receptor-mediated mechanisms.
Authors: Penatti Et al.
J Neurosci 2009;29:12484
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