L-655,708 是一种有效的 α5 亚基选择性 GABAA 受体反向激动剂 (Ki\u003d0.45 nM)。
| Cas No. | 130477-52-0 |
| 化学名 | (S)-ethyl 7-methoxy-9-oxo-11,12,13,13a-tetrahydro-9H-benzo[e]imidazo[5,1-c]pyrrolo[1,2-a][1,4]diazepine-1-carboxylate |
| Canonical SMILES | CCOC(C(N=CN12)=C2[C@]3([H])CCCN3C(C4=C1C=CC(OC)=C4)=O)=O |
| 分子式 | C18H19N3O4 |
| 分子量 | 341.37 |
| 溶解度 | DMF: 2mg/mL,DMF:PBS (pH 7.2) (1:20): 0.04mg/mL,DMSO: 1mg/mL |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | L-655708 is a potent α5 subunit-selective GABAA receptor inverse agonist (Ki = 0.45 nM).IC50: 0.45 nM (Ki)Target: GABAin vitro: L-655708 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 orα6 subunits in combination with β3 and γ2. Enhances LTP in a mouse hippocampal slice model and increases spatial learning, without displaying proconvulsant activity.in vivo: L-655708 at 0.7 mg/kg, administered intraperitoneally, would result in 60-70% occupancy of α5 GABAA receptors with limited binding to α1, α2, and α3 subunit-containing GABAA receptors and no significant off-target behavioral effects, such as sedation and motor impairment.[1] References:
[1]. Saab BJ, et al. Short-term memory impairment after isoflurane in mice is prevented by the α5 γ-aminobutyric acid type A receptorinverse agonist L-655708. Anesthesiology. 2010 Nov;113(5):1061-1071. |
