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编 号:F622125
分子式:C20H34Cl2N2O
分子量:389.4
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生物活性:
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.

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 ratsweighing 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.
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