| Identification | Back Directory | [Name]
JNJ-5207852 dihydrochloride | [CAS]
1782228-76-5 | [Synonyms]
Inhibitor,toxicity,JNJ5207852,inhibit,low,JNJ 5207852,sleep,REM,JNJ-5207852,Histamine Receptor,JNJ5207852 dihydrochloride,JNJ 5207852 dihydrochloride | [Molecular Formula]
C20H33ClN2O | [MDL Number]
MFCD19690931 | [MOL File]
1782228-76-5.mol | [Molecular Weight]
352.95 |
| Hazard Information | Back Directory | [Uses]
JNJ-5207852 dihydrochloride is a selective and potent histamine H3 receptor (H3R) antagonist, with pKis of 8.9, 9.24 for rat and human H3R, respectively. | [in vivo]
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[1]. | Animal Model: | Male, Sprague-Dawley rats weighing 282-334 g[1].
| | Dosage: | 3, 10, 30 mg/kg. | | Administration: | S.C. | | Result: | Iincreased time spent awake and decreased REM sleep and slow-wave sleep. |
| [IC 50]
H3 Receptor: 8.9 (pKi, for rat); H3 Receptor: 9.24 (pKi, for human) | [storage]
Desiccate at RT | [References]
[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. DOI:10.1038/sj.bjp.0705964
[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. DOI:10.3389/fnsys.2012.00054 |
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| Company Name: |
R&D Systems, Inc
|
| Tel: |
18003437475 18003437475 |
| Website: |
www.rndsystems.com |
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