L-655,708
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
Purity: ≥98%
Biological Activity
L-655,708 is a potent, 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. -
Molecular and functional diversity of GABA-A receptors in the enteric nervous system of the mouse colon.
Seifi M, Brown J, Mills J, Bhandari P, Belelli D, Lambert J, Rudolph U, Swinny J
, 2014;0(0):. -
L-655,708 enhances cognition in rats but is not proconvulsant at a dose selective for α5-containing GABAA receptors.
Atack et al.
Neuropharmacology, 2006;51:1023 -
[3H]L-655,708, a novel ligand selective for the benzodiazepine site of GABAA receptors which contain the α5 subunit.
Quirk et al.
Neuropharmacology, 1996;35:1331 -
Rat and human hippocampal α5 subunit-containing γ-aminobutyric acidA receptors have α5α3γ2 pharmacological characteristics.
Sur et al.
Mol.Pharmacol., 1998;54:928
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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
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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.
Pharmacol.Biochem.Behav. 2018;175:139
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GABAA Receptor Subtypes Regulate Stress-Induced Colon Inflammation in Mice.
Authors: Seifi Et al.
Gastroenterology 2018;155:852
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Diminished KCC2 confounds synapse specificity of LTP during senescence.
Authors: Ferando Et al.
Nat Neurosci 2016;19:1197
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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
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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
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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
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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
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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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