H3 receptor:8.9 (pKi, for rat)
H3 receptor:9.24 (pKi, for human)
In Vivo
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].
In Vitro
Kinase Assay
Cell Assay
Animal Administration
Rats[1] Male, Sprague-Dawley rats weighing 282-334 g are used. The animals are individually housed with free access to food and water. To assure that there are no pre-existing group differences in activity levels prior to the initiation of treatment, LMA is monitored and recorded during a 2 h habituation period. Following the 2 h habituation period, testing is briefly interrupted and animals are s.c. injected with either saline (1 mL/kg; n=6), JNJ-5207852 (3, 10, 30 mg/kg; n=6-7 animals/group) or Damphetamine (0.75 mg/kg; n=6). Testing is immediately resumed following the compound injection[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.
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