| 产品描述： | Lorediplon is a novel hypnotic drug acting as a GABAA receptor modulator, differentially active at the α1-subunit, associated with promoting sleep. |
| 靶点： |
GABA Receptor;GABAReceptor |
| 体内研究： |
In vivo, Lorediplon inhibits spontaneous motor activity and increases the duration of sleep in mice (ED50s = 0.13 and 1.2 mg/kg, respectively). It selectively inhibits spontaneous motor activity, which is driven by α1 subunit-containing GABAA receptors, over modification of muscular tone in mice, an α2 subunit-containing GABAA receptor-stimulated activity. Lorediplon (0.13 and 1.2 mg/kg) also decreases latency to slow-wave sleep (SWS) and paradoxical sleep (PS) in mice |
| 参考文献： |
1. Anaclet C, et al. Effects of GF-015535-00, a novel α1 GABA A receptor ligand, on the sleep-wake cycle in mice, with reference to zolpidem. Sleep. 2012 Jan 1;35(1):103-11. 2. Horoszok L, et al. A single-dose, randomized, double-blind, double dummy, placebo and positive-controlled, five-way cross-over study to assess the pharmacodynamic effects of lorediplon in a phase advance model of insomnia in healthy Caucasian adult male subjects. Hum Psychopharmacol. 2014 May;29(3):266-73. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.535 ml |
12.677 ml |
25.354 ml |
| 5 mM |
0.507 ml |
2.535 ml |
5.071 ml |
| 10 mM |
0.254 ml |
1.268 ml |
2.535 ml |
| 50 mM |
0.051 ml |
0.254 ml |
0.507 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京