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.
|Storage||Desiccate at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 341.37. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.93 mL||14.65 mL||29.29 mL|
|5 mM||0.59 mL||2.93 mL||5.86 mL|
|10 mM||0.29 mL||1.46 mL||2.93 mL|
|50 mM||0.06 mL||0.29 mL||0.59 mL|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
References are publications that support the products' biological activity.
Atack et al (2006) L-655,708 enhances cognition in rats but is not proconvulsant at a dose selective for α5-containing GABAA receptors. Neuropharmacology 51 1023 PMID: 17046030
Quirk et al (1996) [3H]L-655,708, a novel ligand selective for the benzodiazepine site of GABAA receptors which contain the α5 subunit. Neuropharmacology 35 1331 PMID: 9014149
Sur et al (1998) Rat and human hippocampal α5 subunit-containing γ-aminobutyric acidA receptors have α5α3γ2 pharmacological characteristics. Mol.Pharmacol. 54 928 PMID: 9804628
If you know of a relevant reference for L-655,708, please let us know.
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Keywords: Selective α5 alpha5 containing a5 GABAA receptors Receptors inverse agonists benzodiazepine L655708 GABAA Receptors
4 Citations for L-655,708
Citations are publications that use Tocris products. Selected citations for L-655,708 include:
Jaiswal et al (2015) Reduction in focal ictal activity following transplantation of MGE interneurons requires expression of the GABAA receptor α4 subunit. J Neurosci 9 127 PMID: 25914623
Seifi et al (2014) Molecular and functional diversity of GABA-A receptors in the enteric nervous system of the mouse colon. Stem Cells Dev 34 10361 PMID: 25080596
Drexler et al (2013) Enhancing the function of alpha5-subunit-containing GABAA receptors promotes action potential firing of neocortical neurons during up-states. Eur J Pharmacol 703 18 PMID: 23380687
Rüedi-Bettschen et al (2013) Modulation of α5 subunit-containing GABAA receptors alters alcohol drinking by rhesus monkeys. Alcohol Clin Exp Res 37 624 PMID: 23126673
Do you know of a great paper that uses L-655,708 from Tocris? If so please let us know.
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