Cat. No. 1327
Chemical Name: 11,12,13,13a-Tetrahydro-7-methoxy-9
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.
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.
Certificate of Analysis / Product Datasheet / Safety Datasheet
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.
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.
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.
If you know of a relevant reference for L-655,708 please let us know.
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.
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Keywords: L-655,708, supplier, Selective, α5, alpha5, containing, a5, GABAA, receptors, Receptors, inverse, agonists, benzodiazepine, L655708, Tocris Bioscience, GABAA Receptor Benzodiazepine products
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