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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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.25 mM||11.72 mL||58.59 mL||117.17 mL|
|1.25 mM||2.34 mL||11.72 mL||23.43 mL|
|2.5 mM||1.17 mL||5.86 mL||11.72 mL|
|12.5 mM||0.23 mL||1.17 mL||2.34 mL|
References are publications that support the biological activity of the product.
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
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Keywords: L-655,708, L-655,708 supplier, Selective, α5, alpha5, containing, a5, GABAA, receptors, Receptors, inverse, agonists, benzodiazepine, L655708, 1327, Tocris Bioscience
8 Citations for L-655,708
Citations are publications that use Tocris products. Selected citations for L-655,708 include:
Seifi et al (2018) GABAA Receptor Subtypes Regulate Stress-Induced Colon Inflammation in Mice. Gastroenterology 155 852 PMID: 29802853
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
Penatti et al (2009) Chronic exposure to anabolic androgenic steroids alters neuronal function in the mammalian forebrain via androgen receptor- and estrogen receptor-mediated mechanisms. J Neurosci 29 12484 PMID: 19812324
Ferando et al (2016) Diminished KCC2 confounds synapse specificity of LTP during senescence. Nat Neurosci 19 1197 PMID: 27500406
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
Xiong et al (2018) 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. Pharmacol.Biochem.Behav. 175 139 PMID: 30359627
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
GABA Receptors Scientific Review
Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.
Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.