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Submit ReviewL-655,708
说明： Benzodiazepine inverse agonist; selective for α5-containing GABAA receptors
化学名： 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
纯度： ≥98% (HPLC)
生物活性 for L-655,708
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.
化合物库 for L-655,708
L-655,708 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for L-655,708
| 分子量 | 341.37 |
| 公式 | C18H19N3O4 |
| 储存 | Desiccate at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 130477-52-0 |
| PubChem ID | 5311203 |
| InChI Key | YKYOQIXTECBVBB-AWEZNQCLSA-N |
| Smiles | O=C(N3[C@]([H])2CCC3)C4=C(C=CC(OC)=C4)N1C2=C(C(OCC)=O)N=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for L-655,708
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 8.53 | 25 |
制备储备液 for L-655,708
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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 |
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产品说明书 for L-655,708
参考文献 for L-655,708
参考文献是支持产品生物活性的出版物。
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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关键词: L-655,708, L-655,708 supplier, Selective, α5, alpha5, containing, a5, GABAA, receptors, Receptors, inverse, agonists, benzodiazepine, L655708, 1327, Tocris Bioscience
8 篇 L-655,708 的引用文献
引用文献是使用了 Tocris 产品的出版物。 L-655,708 的部分引用包括：
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
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
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
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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