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.
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All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
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.
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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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April 10 - 13, 2017