| 产品描述： | JNJ-5207852 is a selective and potent histamine H3 receptor (H3R) antagonist, with pKis of 8.9, 9.24 for rat and human H3R, respectively. |
| 靶点： |
H3 receptor:8.9 (pKi, for rat);H3 receptor:9.24 (pKi, for human) |
| 体内研究： |
JNJ-5207852 (1-10mg/kg s.c.) increases time spent awake and decreases REM sleep and slow-wave sleep, but fails to have an effect on wakefulness or sleep in H3 receptor knockout mice. The wake promoting effects of this H3 receptor antagonist are not associated with hypermotility. A 4-week daily treatment of mice with JNJ-5207852 (10 mg/kg i.p.) does not lead to a change in body weight. JNJ-5207852 is extensively absorbed after oral administration and reaches high brain levels. Animal Model: Male, Sprague-Dawley rats weighing 282-334 g. Dosage: 3, 10, 30 mg/kg. Administration: S.C. Result: Iincreased time spent awake and decreased REM sleep and slow-wave sleep. |
| 参考文献： |
1. Barbier AJ, et al. Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br J Pharmacol. 2004 Nov;143(5):649-61. 2. Abuhamdah RM, et al. Effects of methimepip and JNJ-5207852 in Wistar rats exposed to an open-field with and without object and in Balb/c mice exposed to a radial-arm maze. Front Syst Neurosci. 2012 Jul 16;6:54. |
| 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 |
2.568 ml |
12.84 ml |
25.681 ml |
| 5 mM |
0.514 ml |
2.568 ml |
5.136 ml |
| 10 mM |
0.257 ml |
1.284 ml |
2.568 ml |
| 50 mM |
0.051 ml |
0.257 ml |
0.514 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