JNJ 5207852 dihydrochloride |
| Katalog-Nr.GC11046 |
JNJ 5207852 Dihydrochlorid ist ein selektiver und potenter Antagonist des Histamin-H3-Rezeptors (H3R) mit pKis-Werten von 8,9 bzw. 9,24 fÜr Ratten- bzw. Human-H3R.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 398473-34-2
Sample solution is provided at 25 µL, 10mM.
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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.
In mice and rats, 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. No rebound hypersomnolence, as measured by slow-wave delta power, is observed. 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, possibly due to the compound being a neutral antagonist at the H3 receptor. JNJ-5207852 is extensively absorbed after oral administration and reaches high brain levels[1].
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.
[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.
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)
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